614 results on '"Govindaraj, Saravanan"'
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2. Nanoparticles for diagnosis and treatment of renal diseases
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Kunjiappan, Selvaraj, primary, Panneerselvam, Theivendren, additional, Pandian, Sureshbabu Ram Kumar, additional, Pavadai, Parasuraman, additional, Govindaraj, Saravanan, additional, Ravishankar, Vigneshwaran, additional, Arunachalam, Sankarganesh, additional, and Murugesan, Sankaranarayanan, additional more...
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- 2023
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Catalog
3. Contributors
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Agrawal, Shruti, primary, Ahmad, Shaban, additional, Allawadhi, Prince, additional, Arunachalam, Sankarganesh, additional, Banothu, Anil Kumar, additional, Begum, Shahanaz, additional, Bharani, Kala Kumar, additional, Bhattacharyya, Srirupa, additional, Biswas, Trisha, additional, Chauhan, Lakshita, additional, Chockalingam, S, additional, Cordeiro, Helon Guimarães, additional, Dam, Amrita, additional, Dwivedi, Aradhana, additional, Ferreira, Danilo Roberto Carvalho, additional, Garg, Deepa, additional, Goswami, Mayank, additional, Govindaraj, Saravanan, additional, Jain, Shikha, additional, Sandhu, Kajal, additional, Khan, Fatima Nazish, additional, Khurana, Isha, additional, Khurana, Amit, additional, Kumar, Pramod, additional, Kunjiappan, Selvaraj, additional, Laha, Anindita, additional, Lemos, Moline Severino, additional, Matai, Ishita, additional, Mateti, Tarun, additional, Mehta, Sunita, additional, Murugesan, Sankaranarayanan, additional, Naik, Ramavath Redya, additional, Neeradi, Dinesh, additional, Packirisamy, Gopinath, additional, Pandian, Sureshbabu Ram Kumar, additional, Panneerselvam, Theivendren, additional, Pavadai, Parasuraman, additional, Plaimas, Kitiporn, additional, Qazi, Sahar, additional, Raguraman, Muthuraman, additional, Rajan, Mariappan, additional, Ramlal, Ayyagari, additional, Ravishankar, Vigneshwaran, additional, Raza, Khalid, additional, Sachdev, Abhay, additional, Sadasivam, Rajkumar, additional, Sagar, Kalpana, additional, Sharma, Deepanjali, additional, Thakur, Goutam, additional, Thalugula, Sunitha, additional, Tonelli, Fernanda Maria Policarpo, additional, and Tonelli, Flávia Cristina Policarpo, additional more...
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- 2023
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4. Removal of water and their soluble materials from fuels using Moringa oleifera loaded keratin-co-sodium acrylate hydrogel
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Palanisamy, Ponnusamy, Pavadai, Parasuraman, Arunachalam, Sankarganesh, Pandian, Sureshbabu Ram Kumar, Ravishankar, Vigneshwaran, Govindaraj, Saravanan, Somasundaram, Balasubramanian, Panneerselvam, Theivendren, and Kunjiappan, Selvaraj more...
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- 2021
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5. Optimization and analysis of ultrasound-assisted extraction of bioactive polyphenols from Garcinia indica using RSM and ANFIS modeling and its anticancer activity
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Kunjiappan, Selvaraj, Panneerselvam, Theivendren, Govindaraj, Saravanan, Kannan, Suthendran, Parasuraman, Pavadai, Arunachalam, Sankarganesh, Sankaranarayanan, Murugesan, Baskararaj, Suraj, Palanisamy, Ponnusamy, and Ammunje, Damodar Nayak more...
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- 2020
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6. Formulation and characterization of folate receptor-targeted PEGylated liposome encapsulating bioactive compounds from Kappaphycus alvarezii for cancer therapy
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Baskararaj, Suraj, Panneerselvam, Theivendren, Govindaraj, Saravanan, Arunachalam, Sankarganesh, Parasuraman, Pavadai, Pandian, Sureshbabu Ram Kumar, Sankaranarayanan, Murugesan, Mohan, Uma Priya, Palanisamy, Ponnusamy, Ravishankar, Vigneshwaran, and Kunjiappan, Selvaraj more...
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- 2020
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7. Zika Virus NS5 Protein novel Inhibitors from Limonium sinense phytochemicals using Glide: In silico Approach.
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Shanmugam, Jayaprakash, Govindaraj, Saravanan, Jayaprakash, Geetha, Natarajan, Kiruthiga, and Pandiyan, Balaji
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ZIKA virus ,ZIKA virus infections ,VIRAL proteins ,AEDES albopictus ,QUERCETIN ,AEDES aegypti ,EPIGALLOCATECHIN gallate - Abstract
Zika virus infection causes significant congenital disabilities, in addition to microcephaly while an excited mother is infected during pregnancy. Mosquito vectors are the main spreaders of the zika virus which includes Aedes albopictus and Aedes aegypti. presently clear-cut and definite treatment for the zika virus is not yet available. engrossing in silico approach present study determines the active fighter constituents from aboriginal antiviral herbs to regulate the zika virus. The Lipinski rule filter was used for the Phytoconstituents to determine their molecular interactions and pharmacokinetic studies. NS5 polymerase protein (PDB ID; 5U04) and ligand interactions were determined using Schrodinger Maestro software version 12.7. The outcome displayed that Quercetin, Moupinamide, Epigallocatechin gallate, and Myricetin have sharpened synergism with the asparte active site of NS5 RdRps with docking score (-6.087, -5.838, - 5.812, -5.418 Kcal/mol). Analysing the pharmacokinetic study hydrogen bonds with 2.5 Å for target Aspartate amino acid have prime activity. the present study propounds that Quercetin can be used as an inhibitor of the Zika virus. [ABSTRACT FROM AUTHOR] more...
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- 2024
8. A review on Artificial Intelligence Approaches and Rational approaches in Drug Discovery
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Kunjiappan, Selvaraj, primary, Pavadai, Parasuraman, primary, Srivathsa, Anjana Vidya, additional, Sadashivappa, Nandini Markuli, additional, Hegde, Apeksha K, additional, Radha, Srimathi, additional, Mahesh, Agasa Ramu, additional, Ammunje, Damodar Nayak, additional, Sen, Debanjan, additional, Panneerselvam, Theivendren, additional, and Govindaraj, Saravanan, additional more...
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- 2023
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9. Synthesis, characterization and in vitro antimicrobial activity of some 1-(substitutedbenzylidene)-4-(4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)phenyl)semicarbazide derivatives
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Govindaraj Saravanan, Veerachamy Alagarsamy, and Chinnasamy Rajaram Prakash
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Quinazolin-4(3H)-one ,Semicarbazide ,Schiff base ,Antibacterial activity ,Antifungal activity ,Chemistry ,QD1-999 - Abstract
A series of 1-(substitutedbenzylidene)-4-(4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl) phenyl)semicarbazide derivatives were synthesized with the aim of developing potential antimicrobials. It was characterized by FT-IR, 1H NMR, Mass spectroscopy and elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique and agar streak dilution method. All title compounds showed activity against the entire strain of microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds were well discussed. Based on the results obtained, compound 5j was found to be very active compared to the rest of the compounds which were subjected to antimicrobial assay. more...
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- 2015
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10. Graph Theoretical analysis, in silico modeling and molecular dynamic studies of (5-((2-chloropyridin-4-yl)oxy)-3-phenyl-1H-pyrazol-1-yl)-2-(4-substituted phenyl)-N,N-dimethylethen-1-amine derivatives for the treatment of breast cancer
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Panneerselvam, Theivendren, primary, Kunjiappan, Selvaraj, additional, Govindaraj, Saravanan, additional, Gopal, Murugananthan, additional, Natarajan, Kiruthiga, additional, Hegde, Yashoda Mariappa, additional, Shanmugam, Nivetha, additional, Srinivas, Geetha, additional, Ravi, Kaveena, additional, and Natarajan, Vignesh, additional more...
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- 2022
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11. Chapter 4 - Nanoparticles for diagnosis and treatment of renal diseases
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Kunjiappan, Selvaraj, Panneerselvam, Theivendren, Pandian, Sureshbabu Ram Kumar, Pavadai, Parasuraman, Govindaraj, Saravanan, Ravishankar, Vigneshwaran, Arunachalam, Sankarganesh, and Murugesan, Sankaranarayanan more...
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- 2023
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12. Microwave-assisted synthesis, characterization and biological activity of novel pyrazole derivatives
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Theivendren Panneer Selvam, Palanirajan Vijayaraj Kumar, Govindaraj Saravanan, and Chinnasamy Rajaram Prakash
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Pyrazole ,Anti-inflammatory activity ,Analgesic activity ,Chemistry ,QD1-999 - Abstract
A series of 1-(4-substitutedphenyl)-3-phenyl-1H-pyrazole-4-carbaldehydes 4a–l have been synthesized and tested for their biological activities. Formation of the pyrazole derivatives was achieved by treating with Vilsmeier-Haack reagent. The newly synthesized compounds were evaluated for their anti-inflammatory and analgesic activities compared to Diclofenac sodium as standard drug. Compounds 4g, 4i and 4k exhibited the maximum anti-inflammatory and analgesic activities. The detailed synthesis, spectroscopic and toxicity data are reported. more...
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- 2014
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13. Anticonvulsant activity of novel 1-(morpholinomethyl)-3-substituted isatin derivatives
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Govindaraj Saravanan, Veerachamy Alagarsamy, and Pandurangan Dineshkumar
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Epilepsy ,In vivo studies ,Isatin ,Isoxazole ,Morpholine ,Therapeutics. Pharmacology ,RM1-950 ,Pharmacy and materia medica ,RS1-441 ,Pharmaceutical industry ,HD9665-9675 - Abstract
A variety of novel isatin derivatives 5a–5j and 6a–6j were synthesized and characterized by spectroscopic means and elemental analysis. The title compounds were investigated for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by the rotorod test. The relationship between the functional group variation and the biological activity of the evaluated compounds was discussed. Among the synthesized analogs, the most active one was 6f that revealed protection in MES at a dose of 30 mg/kg (i.p.) after 0.5 h and 4 h. This molecule also provided protection in the scPTZ at a dose of 100 mg/kg (0.5 h) and 300 mg/kg (4 h). more...
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- 2014
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14. Synthesis, characterization and antimicrobial activity of some novel benzimidazole derivatives
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Immadisetty Sri Krishnanjaneyulu, Govindaraj Saravanan, Janga Vamsi, Pamidipamula Supriya, Jarugula Udaya Bhavana, and Mittineni Venkata Sunil Kumar
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Antibacterial ,antifungal ,chalcone ,mannich base ,pyrazole ,Therapeutics. Pharmacology ,RM1-950 ,Pharmacy and materia medica ,RS1-441 - Abstract
A series of novel N-((1H-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-substituted-4, 5-dihydro-1-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-substituted-4, 5-dihydro-1H-pyrazol-3-yl) benzenamine were synthesized by treating various 1-(4-((1H-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one with phenyl hydrazine in the presence of sodium acetate through a simple ring closure reaction. The starting material, 1-(4-((1H-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one,-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one, was synthesized from o-phenylenediamine by a multistep synthesis. All the synthesized compounds were characterized by spectroscopic means and elemental analyses. The title compounds were investigated for in vitro antibacterial and antifungal properties against some human pathogenic microorganisms by employing the agar streak dilution method using Ciprofloxacin and Ketoconazole as standard drugs. All title compounds showed activity against the entire strains of microorganism. Structural activity relationship studies reveal that compounds possessing an electron-withdrawing group display better activity than the compounds containing electron-donating groups, whereas the unsubstituted derivatives display moderate activity. Based on the results obtained, N-((1H-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-(4-(trifluoromethyl) phenyl)-4,5-dihydro-1H-pyrazol-3-yl) benzenamine 5i was found to be very active compared with the rest of the compounds and standard drugs that were subjected to antimicrobial assay. more...
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- 2014
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15. Anti-HIV and Antibacterial Activities of Novel 2-(3-Substituted-4-oxo-3,4-dihydroquinazolin-2-yl)-2,3-dihydrophthalazine-1,4-diones
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K. Chitra, V. Raja Solomon, Veerachamy Alagarsamy, Govindaraj Saravanan, and M. T. Sulthana
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0301 basic medicine ,Phthalic anhydride ,010405 organic chemistry ,Anti hiv ,Organic Chemistry ,Agar Dilution Method ,Antimicrobial ,01 natural sciences ,Biochemistry ,Combinatorial chemistry ,0104 chemical sciences ,03 medical and health sciences ,chemistry.chemical_compound ,030104 developmental biology ,chemistry ,Antibacterial activity ,EC50 - Abstract
In the present study, we have synthesized a series of novel 2-(3-substituted-4-oxo-3,4-dihydroquinazolin-2-yl)-2,3-dihydrophthalazine-1,4-diones by the reaction of 3-(substituted)-2-hydrazino-quinazoline-4(3H)-ones with phthalic anhydride. The starting material 3-(substituted)-2-hydrazino-quinazolin-4(3H)-ones were synthesized from various primary amines. All the synthesized compounds were screened for their antitubercular, anti-HIV and antibacterial activity against different gram positive and gram negative strains by agar dilution method. Among the test compounds, 2-(3-(4-chlorophenyl)-4-oxo-3,4-dihydroquinazolin-2-yl)-2,3-dihydrophthalazine-1,4-dione (QCT7) shown most potent antibacterial activity against E. coli, and S. aureus with the MIC of 3 µg/mL. The compound QCT7 exhibited the antitubercular activity with the MIC of 25 µg/mL and anti-HIV activity with the EC50 of 43.68 µM against HIV1 and HIV2 and offers potential lead for further optimization and development to new antitubercular and anti-HIV agents. The results obtained from this study confirm that the synthesized and biologically evaluated quinazolines showed promising antimicrobial, antitubercular and anti-HIV activities and are new scaffolds for antimicrobial activity. more...
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- 2021
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16. An Efficient Design of 16 Bit MAC Unit using Vedic Mathematics
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N. Manoj Kumar, D. Shyam Ganesh, S. Kanimozi, and Govindaraj Saravanan
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16-bit ,Hardware_ARITHMETICANDLOGICSTRUCTURES ,Arithmetic ,Unit (ring theory) ,Mathematics - Abstract
Duplicate and Accumulate (MAC) is one of the central practices utilized absolutely in signal- controlling and different applications. The multiplier is the major piece of Digital Signal Processors (DSPs). Its cutoff spins around power, LUT use, and surrender pick the presence of a DSP. In like way, there is a need to sort out the drive and give up fit multiplier. In this paper, a 16-digit MAC unit is proposed to utilize an 8-cycle Vedic multiplier and pass on a save snake. A relationship with the current 8-cycle Vedic multiplier utilizing Square-Root (SQR) Carry-select snake (CSLA) is introduced. It is isolated and a standard pack multiplier. The whole technique is done in Verilog HDL. Blend and redirections were finished utilizing Xilinx InDesign Suite 14.5. The proposed game plan accomplishes fundamental improvement in region and suspension. In like manner, an abatement in power around 9.5% is refined. more...
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- 2021
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17. Graph Theoretical analysis and in silico modeling and molecular dynamic studies of fused indolin-2-one derivatives for the treatment of inflammation
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Theivendren, Panneerselvam, primary, Kunjiappan, Selvaraj, additional, Pavadai, Parasuraman, additional, Govindaraj, Saravanan, additional, Gopal, Murugananthan, additional, Pachiappan, Sudhakar, additional, Hegde, Yashoda Mariappa, additional, and Shanmugam, Nivetha, additional more...
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- 2022
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18. Synthesis of piperidine-4-one Derivative Containing Dipeptide: An Acetyl cholinesterase and β-secretase Inhibitor
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Vasudevan Mani, Veerachamy Alagarsamy, Damodar Nayak Ammunje, Jithendra Chimakurthy, Theivendren Panneerselvam, Selvaraj Kunjiappan, Govindaraj Saravanan, Parasuraman Pavadai, Suresh Ramalingam, and Pandurangan Perumal more...
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Pharmacology ,030506 rehabilitation ,Dipeptide ,Stereochemistry ,05 social sciences ,03 medical and health sciences ,chemistry.chemical_compound ,Infectious Diseases ,chemistry ,β secretase ,0501 psychology and cognitive sciences ,Acetyl cholinesterase ,Piperidine ,0305 other medical science ,Derivative (chemistry) ,050104 developmental & child psychology - Abstract
Background: With the goal of developing Alzheimer's disease therapeutics, we have designed and synthesized novel piperidone fused dipeptide (DPPS) derivatives possessing dual action such as acetylcholinesterase (AChE) and beta-amyloid peptide (Aβ) aggregation inhibition. Designed peptide was synthesized by solid phase peptide synthesis using FMOC chemistry protocol and characterized by mass spectroscopy. Methods: The amino acid sequence in peptide was analyzed by LC-MS-MS. In silico docking analysis was carried out using GLIDE software. The docking score using GLIDE was found to be -7.88 against AChE and -9.74 against BACE1 enzyme. In vitro enzyme inhibition assay was carried out for AChE enzyme and BACE1 enzyme. Results: The IC50 values of AChE inhibition and BACE1 of DPPS were found to be 0.4796 μM/ml and 0.0154 μM/ml, respectively. The correlation of in silico and in vitro results showed that DPPS possessed a greater ability to inhibit BACE1 enzyme. more...
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- 2020
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19. Design, Optimization, Synthesis and AntiTB Screening of Benzimidazole Derivatives
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Pavadai Parasuraman, Veerachamy Alagarsamy, Govindaraj Saravanan, Theivendren Panneerselvam, and Selvaraj Kunjiappan
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Pharmacology ,Benzimidazole ,chemistry.chemical_compound ,Infectious Diseases ,010405 organic chemistry ,Chemistry ,010402 general chemistry ,01 natural sciences ,Combinatorial chemistry ,0104 chemical sciences - Abstract
Introduction: A biologically active benzimidazole synthesis was carried out at laboratory scale in order to reduce environmental pollution as well as to identify effective synthetic route. Methods: In this connection optimization was performed by Central Composite Rotatable Design (CCRD) to develop experimental data through Response Surface Methodology (RSM). The optimization of title analogue was performed by RSM which led us to the identification of high quality of synthetic yield. The effects of four independent parameters [1-5 mol of oxobutanoic acid (X1), 1-5 mol of thionyl chloride (X2), 1-5 mol of imidazol-2-yl-4-oxobutanoyl chloride (X3), and 1-5 mol of 4-nitro aniline (X4) were taken into optimize the synthetic yields of title scaffold. Results and Conclusion: A result of randomly generated benchmark and real values such as percentage yield, λmax and Retention Time (RT) of title compound are found to be highly significant. The present model is connected to maximize the percentage yield of title scaffold with the developed optimal set. The highly significant benzimidazole was screened for its MTB activity against MTB H37Ra strain by MABA screening. more...
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- 2020
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20. Synthesis and anti-microbial screening of novel schiff bases of 3-amino-2-methyl quinazolin 4-(3H)-one
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Govindaraj Saravanan, Perumal Pannerselvam, and Chinnasamy Rajaram Prakash
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3-amino-2-methyl quinazolin-4-(3H)-one ,anti-bacterial ,anti-fungal ,Schiff base ,Therapeutics. Pharmacology ,RM1-950 ,Pharmacy and materia medica ,RS1-441 - Abstract
In the present study, novel Schiff bases were synthesized by condensation of 3-amino-2-methyl quinazolin-4-(3H)-ones with different aromatic aldehydes. The 3-amino-2-methyl quinazolin-4-(3H)-one was synthesized from anthranilic acid via the 2-methyl benzoxazin-4-one. The chemical structures of the synthesized compounds were confirmed by means of Infrared (IR), 1 H-NMR, 13 C-NMR, Mass spectral, and Elemental analysis. These compounds were screened for anti-bacterial (Staphylococcus aureus ATCC 9144, Staphylococcus epidermidis ATCC 155, Micrococcus luteus ATCC 4698, Bacillus cereus ATCC 11778, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 2853, and Klebsiella pneumoniae ATCC 11298)) and anti-fungal (Aspergillus niger ATCC 9029 and Aspergillus fumigatus ATCC 46645) activities, using the paper disk diffusion technique. The minimum inhibitory concentrations (MIC) of the compounds were also determined by the agar streak dilution method. Most of the synthesized compounds exhibited significant anti-bacterial and anti-fungal activities. Among the synthesized compounds, 3-(4-hydroxy benzylideneamino)-2-methyl quinazolin-4(3H)-one 4g and 4c was found to exhibit the highest anti-bacterial activity and 3-(4-hydroxy-3-methoxy benzylideneamino)-2-methyl quinazolin-4(3H)-one 4k exhibited the highest anti-fungal activity. more...
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- 2010
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21. Dendrimers as a Novel Carrier in Anti-HIV Therapy
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P. Arshad, Pandurangan Dineshkumar, K. Naga Jyothi, M. Karthik, and Govindaraj Saravanan
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virus diseases ,Anti-HIV Therapy ,Virology - Abstract
The present treatments for HIV transfection include chemical agents and gene therapies. Although many chemical drugs, peptides and genes have been developed for HIV inhibition, a variety of non-ignorable drawbacks limited the efficiency of these materials. Dendrimers has ability to carrier of antiviral drugs due to some properties such as mono-dispersity, defined structure, amenability for functionalization using diverse ligands and its low-nanometer size. In this review, we discuss the application of dendrimers as both therapeutic agents and non-viral vectors of chemical agents and genes for HIV treatment. In one way, dendrimers with functional end groups combine with the gp120 of HIV and CD4 molecule of host cell to suppress the attachment of HIV to the host cell. In another way, dendrimers are also able to transfer chemical drugs and genes into the host cells, which increase the anti-HIV activity of these materials. Dendrimers as therapeutic tools provide a potential treatment for HIV infection. Keywords: Dendrimers, Drug release, Drug targeting, gp120, CD4, Antiviral drug more...
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- 2019
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22. Graph theoretical analysis, in silico modeling, prediction of toxicity, metabolism and synthesis of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl) phenyl) quinazolin-4(3H )-ones as NMDA receptor inhibitor
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Theivendren Panneerselvam, Pavadai Parasuraman, Selvaraj Kunjiappan, Veerachamy Alagarsamy, Govindaraj Saravanan, Suresh Ramalingam, Damodar Nayak Ammunje, Shrinivas D. Joshi, Padmaja Udayakumar, and Muthukrishnan Soundararajan more...
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Male ,Stereochemistry ,Neurotoxicity ,Oxadiazole ,Models, Theoretical ,Ligand (biochemistry) ,medicine.disease ,Receptors, N-Methyl-D-Aspartate ,Mice ,chemistry.chemical_compound ,chemistry ,Seizures ,Rotarod Performance Test ,Drug Discovery ,Toxicity ,Quinazoline ,medicine ,Animals ,NMDA receptor ,Potency ,Anticonvulsants ,Computer Simulation ,Rats, Wistar ,Receptor ,Quinazolinones - Abstract
Hit, Lead & Candidate Discovery A variety of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl)phenyl) quinazolin-4(3H)-ones have been synthesized by treating 3-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl)-2-(methyl/phenyl)-quinazolin-4(3H)-one with a variety of secondary amines. Graph theoretical analysis was used in identification of drug target that is, NMDAR (N-methyl-d-aspartate receptors). The observed reports of in silico modeling and ligand based toxicity, metabolism prediction studies were encouraging us to synthesize of title compounds and evaluate their antiepileptic effects. The title compounds were tested for its antiepileptic potency by MES and scPTZ model. Rotorod test is used to assess its neurotoxicity. In the preliminary test it was found that in MES test, analogs 6d, 6e, 6f, and 6l were potent; whereas in scPTZ test analogs 6d, 6e, 6f, and 6k displayed potent antiepileptic activity. Additionally these five derivatives were tested in rats orally at a dose of 30 mg/kg and found that compounds 2-methyl-3-(4-(5-morpholino-1,3,4-oxadiazol-2-yl)phenyl)quinazolin-4(3H)-one 6e and 2-methyl-3-(4-(5-(piperidin-1-yl)-1,3,4-oxadiazol-2-yl)phenyl)quinazolin-4(3H)-one 6f exhibited superior activity than reference Phenytoin. In MES test, these derivatives 6e and 6f showed activity at 30 mg/kg i.p. dose after 0.5 hr and 4.0 hr. In scPTZ test these derivatives 6e and 6f showed activity at 100 and 300 mg/kg i.p. dose after 0.5 hr and 4.0 hr, respectively. more...
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- 2019
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23. IMG-20210209-WA0004
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Govindaraj Saravanan, Panneerselvam Theivendren, and Murugananthan Gopal
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- 2021
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24. Nano Based Approach for the Treatment of Neglected Tropical Diseases
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Pandian, Sureshbabu Ram Kumar, primary, Panneerselvam, Theivendren, additional, Pavadai, Parasuraman, additional, Govindaraj, Saravanan, additional, Ravishankar, Vigneshwaran, additional, Palanisamy, Ponnusamy, additional, Sampath, Muthukumar, additional, Sankaranarayanan, Murugesan, additional, and Kunjiappan, Selvaraj, additional more...
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- 2021
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25. Design, graph theoretical analysis, density functionality theories, Insilico modeling, synthesis, characterization and biological activities of novel thiazole fused quinazolinone derivatives
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Veerachamy Alagarsamy, Govindaraj Saravanan, Theivendren Panneerselvam, Pandurangan Dinesh Kumar, Selvaraj Kunjiappan, Pavadai Parasuraman, and Indhumathy Murugan
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Drug ,media_common.quotation_subject ,In silico ,01 natural sciences ,Mice ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Drug Discovery ,Animals ,Humans ,Computer Simulation ,KEGG ,Thiazole ,Quinazolinone ,Quinazolinones ,media_common ,Epilepsy ,Biological studies ,010405 organic chemistry ,Biological activity ,Drug interaction ,Combinatorial chemistry ,Rats ,0104 chemical sciences ,Molecular Docking Simulation ,Thiazoles ,chemistry ,Drug Design ,Anticonvulsants ,030217 neurology & neurosurgery - Abstract
Hit, Lead & Candidate Discovery A series of 2-(2-substituted benzylidenehydrazinyl-2-oxopropyl)-3-(4-[4-oxo-2-phenylthiazolo din-3-yl]phenyl)quinazolin-4(3H)-one 7a-7l were synthesized and characterized by IR, 1 H-NMR, 13 C-NMR, mass spectroscopy and elemental analyses. In this present study, the density functionality theory was performed to identify drug stability. Further we introduced graph theoretical analysis by utilised Kyoto Encyclopedia of Genes and Genomes (KEGG) database and Cytoscape software to identify drug target. Based on the observed drug target insilico modeling was executed to know effective drug. The antiepileptic effects of title compounds were evaluated by using MES and subcutaneous pentylenetetrazole (scPTZ) test. Acute neurological toxicity of title compounds was studied by using standardized rotorod test. After 0.5 hr of period many of the compounds showed anticonvulsant activity at MES or scPTZ test. Comparison of the biological activity of test compounds with its chemical structures indicates that, compounds possessing electron donating group exhibited superior activity than the analogs having electron withdrawing moieties. Among the electron donating group tested, amino derivative exhibited good activity than rest of derivatives. From the study it was concluded that, the compound 7j was established as very potent compared with rest of the compounds and standard drugs subjected to biological studies. Thus the compound 2-(2-[4-aminobenzylidene]hydrazinyl-2-oxopropyl)-3-(4-[4-oxo-2-phenylthiazolidin-3-yl]phenyl) quinazolin-4(3H)-one (7j) came out as pilot derivative without any neurotoxicity with a wide spectrum of antiepileptic activity. HIGHLIGHTS: The performed work is having great significance in terms of Graph theoretical analysis used to identify drug target In silico modeling used to identify designed drug interaction with identify target Density functionality studies used to identify synthesized compound energy band gap which is correlate with enhancement of its biological activity Antiepileptic effects of entire synthesized quinazolinone scaffolds were evaluated by MES and scPTZ test 2-(2-[4-aminobenzylidene]hydrazinyl-2-oxopropyl)-3-(4-[4-oxo-2-phenylthiazolidin-3-yl]phenyl) quinazolin-4(3H)-one (7j) was established as very potent compared to the rest of the compounds and standard drugs which were subjected to biological studies. more...
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- 2018
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26. Surface receptor‐mediated targeted drug delivery systems for enhanced cancer treatment: A state‐of‐the‐art review
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Kunjiappan, Selvaraj, primary, Pavadai, Parasuraman, additional, Vellaichamy, Sivakumar, additional, Ram Kumar Pandian, Sureshbabu, additional, Ravishankar, Vigneshwaran, additional, Palanisamy, Ponnusamy, additional, Govindaraj, Saravanan, additional, Srinivasan, Gowshiki, additional, Premanand, Adhvitha, additional, Sankaranarayanan, Murugesan, additional, and Theivendren, Panneerselvam, additional more...
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- 2020
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27. Design, in silico modelling and functionality theory of folate-receptor-targeted myricetin-loaded bovine serum albumin nanoparticle formulation for cancer treatment
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Kunjiappan, Selvaraj, primary, Govindaraj, Saravanan, additional, Parasuraman, Pavadai, additional, Sankaranarayanan, Murugesan, additional, Arunachalam, Sankarganesh, additional, Palanisamy, Ponnusamy, additional, Mohan, Uma Priya, additional, Babkiewicz, Ewa, additional, Maszczyk, Piotr, additional, Vellaisamy, Sivakumar, additional, and Panneerselvam, Theivendren, additional more...
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- 2020
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28. Design, In Silico Modelling, and Functionality Theory of Novel Folate Receptor Targeted Rutin Encapsulated Folic Acid Conjugated Keratin Nanoparticles for Effective Cancer Treatment
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Kunjiappan, Selvaraj, primary, Panneerselvam, Theivendren, additional, Govindaraj, Saravanan, additional, Parasuraman, Pavadai, additional, Baskararaj, Suraj, additional, Sankaranarayanan, Murugesan, additional, Arunachalam, Sankarganesh, additional, Babkiewicz, Ewa, additional, Jeyakumar, Aarthi, additional, and Lakshmanan, Muthulakshmi, additional more...
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- 2020
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29. Modeling a pH-sensitive Zein-co-acrylic acid hybrid hydrogels loaded 5-fluorouracil and rutin for enhanced anticancer efficacy by oral delivery
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Bathrinath Sankaranarayanan, Govindaraj Saravanan, Murugesan Sankaranarayanan, Panneerselvam Theivendran, Jawahar Natarajan, Balasubramanian Somasundaram, Suraj Baskararaj, Ponnusamy Palanisamy, Sankarganesh Arunachalam, Selvaraj Kunjiappan, and Ashish Wadhwani more...
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Biocompatibility ,Intrinsic viscosity ,Environmental Science (miscellaneous) ,Biodegradation ,Agricultural and Biological Sciences (miscellaneous) ,Controlled release ,chemistry.chemical_compound ,Rutin ,chemistry ,Polymerization ,Self-healing hydrogels ,Biotechnology ,Nuclear chemistry ,Acrylic acid - Abstract
The combination of natural and synthetic polymeric materials grafted hydrogels offer great potential as oral therapeutic systems because of its intrinsic biocompatibility, biodegradability, protect labile drugs from metabolism and controlled release properties. Hence, in the present study, we aimed to prepare and optimize oral delivered pH-responsive Zein-co-acrylic acid hydrogels incorporated with 5-fluorouracil (5-Fu) and rutin (Ru) for effective anticancer activity with less toxicity. In this study, graft polymerization technique is adopted to formulate hydrogels with various ratios of Zein, acrylic acid, N, N-methylene bisacrylamide, and ammonium persulphate as an initiator. The optimized formulation was identified based on the cross-linking, chemical interactions, intrinsic viscosity (η), dynamic swelling (Q) at pH 1.2, diffusion coefficient (D), sol–gel fraction (%), and porosity (%). The selected optimized formulation has shown significant improvement in drugs loading and encapsulation efficiency, releasing at pH 1.2 and pH 7.4. Drug release kinetics studies confirmed the controlled release properties of hydrogels. Hydrogels were porous and the drug loading of 5-Fu and Ru was found to be 12.13% and 10.86%, respectively, whereas encapsulation efficiency of 5-Fu and Ru was 89.35% and 81.47%, respectively. Furthermore, form the in vitro cytotoxic screening, it was found that 52.5 µg mL−1 5-Fu and Ru-loaded hydrogel impacted 50% of cell death at 24 h, there by significantly arresting the proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines. Altogether, the optimized pH-responsive hydrogels make them favorable carrier for anticancer drugs for oral delivery. more...
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- 2019
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30. Modeling a pH-sensitive Zein
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Selvaraj, Kunjiappan, Panneerselvam, Theivendran, Suraj, Baskararaj, Bathrinath, Sankaranarayanan, Ponnusamy, Palanisamy, Govindaraj, Saravanan, Sankarganesh, Arunachalam, Murugesan, Sankaranarayanan, Jawahar, Natarajan, Balasubramanian, Somasundaram, and Ashish, Wadhwani more...
- Subjects
Original Article - Abstract
The combination of natural and synthetic polymeric materials grafted hydrogels offer great potential as oral therapeutic systems because of its intrinsic biocompatibility, biodegradability, protect labile drugs from metabolism and controlled release properties. Hence, in the present study, we aimed to prepare and optimize oral delivered pH-responsive Zein-co-acrylic acid hydrogels incorporated with 5-fluorouracil (5-Fu) and rutin (Ru) for effective anticancer activity with less toxicity. In this study, graft polymerization technique is adopted to formulate hydrogels with various ratios of Zein, acrylic acid, N, N-methylene bisacrylamide, and ammonium persulphate as an initiator. The optimized formulation was identified based on the cross-linking, chemical interactions, intrinsic viscosity (η), dynamic swelling (Q) at pH 1.2, diffusion coefficient (D), sol–gel fraction (%), and porosity (%). The selected optimized formulation has shown significant improvement in drugs loading and encapsulation efficiency, releasing at pH 1.2 and pH 7.4. Drug release kinetics studies confirmed the controlled release properties of hydrogels. Hydrogels were porous and the drug loading of 5-Fu and Ru was found to be 12.13% and 10.86%, respectively, whereas encapsulation efficiency of 5-Fu and Ru was 89.35% and 81.47%, respectively. Furthermore, form the in vitro cytotoxic screening, it was found that 52.5 µg mL(−1) 5-Fu and Ru-loaded hydrogel impacted 50% of cell death at 24 h, there by significantly arresting the proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines. Altogether, the optimized pH-responsive hydrogels make them favorable carrier for anticancer drugs for oral delivery. more...
- Published
- 2018
31. Optimization and analysis of ultrasound-assisted extraction of bioactive polyphenols from Garcinia indica using RSM and ANFIS modeling and its anticancer activity
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Kunjiappan, Selvaraj, primary, Panneerselvam, Theivendren, additional, Govindaraj, Saravanan, additional, Kannan, Suthendran, additional, Parasuraman, Pavadai, additional, Arunachalam, Sankarganesh, additional, Sankaranarayanan, Murugesan, additional, Baskararaj, Suraj, additional, Palanisamy, Ponnusamy, additional, and Ammunje, Damodar Nayak, additional more...
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- 2019
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32. Design and in silico modeling of Indoloquinoxaline incorporated keratin nanoparticles for modulation of glucose metabolism in 3T3‐L1 adipocytes
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Kunjiappan, Selvaraj, primary, Theivendren, Panneerselvam, additional, Pavadai, Parasuraman, additional, Govindaraj, Saravanan, additional, Sankaranarayanan, Murugesan, additional, Somasundaram, Balasubramanian, additional, Arunachalam, Sankarganesh, additional, Ram Kumar Pandian, Sureshbabu, additional, and Ammunje, Damodar Nayak, additional more...
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- 2019
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33. Synthesis, characterization and in vitro antimicrobial activity of some 1-(substitutedbenzylidene)-4-(4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)phenyl)semicarbazide derivatives
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Veerachamy Alagarsamy, Chinnasamy Rajaram Prakash, and Govindaraj Saravanan
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Semicarbazide ,food.ingredient ,Schiff base ,Chemistry(all) ,Quinazolin-4(3H)-one ,Biological activity ,General Chemistry ,Antimicrobial ,In vitro ,lcsh:Chemistry ,chemistry.chemical_compound ,food ,chemistry ,lcsh:QD1-999 ,Proton NMR ,Organic chemistry ,Agar ,Antibacterial activity ,Antifungal activity ,Nuclear chemistry - Abstract
A series of 1-(substitutedbenzylidene)-4-(4-(2-(methyl/phenyl)-4-oxoquinazolin-3(4 H )-yl) phenyl)semicarbazide derivatives were synthesized with the aim of developing potential antimicrobials. It was characterized by FT-IR, 1 H NMR, Mass spectroscopy and elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique and agar streak dilution method. All title compounds showed activity against the entire strain of microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds were well discussed. Based on the results obtained, compound 5j was found to be very active compared to the rest of the compounds which were subjected to antimicrobial assay. more...
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- 2015
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34. Surface receptor‐mediated targeted drug delivery systems for enhanced cancer treatment: A state‐of‐the‐art review.
- Author
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Kunjiappan, Selvaraj, Pavadai, Parasuraman, Vellaichamy, Sivakumar, Ram Kumar Pandian, Sureshbabu, Ravishankar, Vigneshwaran, Palanisamy, Ponnusamy, Govindaraj, Saravanan, Srinivasan, Gowshiki, Premanand, Adhvitha, Sankaranarayanan, Murugesan, and Theivendren, Panneerselvam more...
- Subjects
TARGETED drug delivery ,DRUG delivery systems ,CANCER treatment ,DNA damage ,DNA repair ,RADIOTHERAPY - Abstract
Enhanced cancer treatment remains as one of the focused areas for researchers around the world. Hence, the progress in this direction will be a challenge and an opportunity in, inter‐disciplinary field to mitigate the suffering of millions in the upcoming decades. As we see, cancer death rate has also progressively increased despite the current impressive treatment regimens but also due to the non‐availability of vaccines and the re‐occurring of cancer in substantially recovered patients. Currently, numerous treatment strategies like surgical removal of solid tumors followed by radiation with a combination of immunotherapy/chemotherapy by the researchers and clinicians are routinely being followed. However, recurrence and distant metastasis often occur following radiation therapy, commonly due to the generation of radio‐resistance through deregulation of the cell cycle, cell death, and inhibition of DNA damage repair mechanisms. Thus, chemotherapeutic/immunotherapeutic treatment systems have progressed remarkably in the latest years owing to destroying tumors, noninvasive, and affordable charge of therapy. But, traditional chemotherapeutic approaches target the DNA of mutated and normal healthy cells, resulting in a significantly increased risk of toxicity and drug resistance. Thus, many receptors targeted therapies are in the developmental phase of discovery. Cancer cells have a specialized set of surface receptors that provide potential targets for cancer therapeutics. Cell surface receptor‐dependent endocytosis is well a known major mechanism for the internalization of macromolecular drugs. This review emphasizes the recent development of several surface receptors mediated cancer‐targeting approaches for the effective delivery of various therapeutic formulations. [ABSTRACT FROM AUTHOR] more...
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- 2021
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35. Graph Theoretical Analysis, In Silico Modeling, Synthesis, Anti-Microbial and Anti-TB Evaluation of Novel Quinoxaline Derivatives
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Shrinivas D. Joshi, Govindaraj Saravanan, Theivendren Panneer Selvam, Pandurangan Dinesh Kumar, Murugan Indhumathy, Veerachamy Alagarsamy, and Selvaraj Kunjiappan
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0301 basic medicine ,Stereochemistry ,In silico ,Antitubercular Agents ,Microbial Sensitivity Tests ,01 natural sciences ,Mycobacterium tuberculosis ,Serine ,03 medical and health sciences ,chemistry.chemical_compound ,Structure-Activity Relationship ,Quinoxaline ,Anti-Infective Agents ,Quinoxalines ,Drug Discovery ,Computer Simulation ,Threonine ,Schiff base ,biology ,Dose-Response Relationship, Drug ,010405 organic chemistry ,Chemistry ,Biological activity ,General Medicine ,Models, Theoretical ,biology.organism_classification ,0104 chemical sciences ,030104 developmental biology ,Acetamide - Abstract
Background We designed to synthesize a number of 2-(2-(substituted benzylidene) hydrazinyl)-N-(4-((3-(phenyl imino)-3,4-dihydro quinoxalin-2(1 H)-ylidene)amino) phenyl) acetamide S1-S13 with the hope to obtain more active and less toxic anti-microbial and anti-TB agents. Methods A series of novel quinoxaline Schiff bases S1-S13 were synthesized from o-phenylenediamine and oxalic acid by a multistep synthesis. In present work, we are introducing graph theoretical analysis to identify drug target. In the connection of graph theoretical analysis, we utilised KEGG database and Cytoscape software. All the title compounds were evaluated for their in-vitro anti-microbial activity by using agar well diffusion method at three different concentration levels (50, 100 and 150 µg/ml). The MIC of the compounds was also determined by agar streak dilution method. Results The identified study report through graph theoretical analysis were highlights that the key virulence factor for pathogenic mycobacteria is a eukaryotic-like serine/threonine protein kinase, termed PknG. All compounds were found to display significant activity against entire tested bacteria and fungi. In addition the synthesized scaffolds were screened for their in vitro antituberculosis (anti-TB) activity against Mycobacterium tuberculosis (Mtb) strain H37Ra using standard drug Rifampicin. Conclusion A number of analogs found markedly potent anti-microbial and anti-TB activity. The relationship between the functional group variation and the biological activity of the evaluated compounds were well discussed. The observed study report was showing that the compound S6 (4-nitro substitution) exhibited most potent effective anti-microbial and anti-TB activity out of various tested compounds. more...
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- 2017
36. An overview of quinazolines: Pharmacological significance and recent developments
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K. Chitra, Bandi Narendhar, Govindaraj Saravanan, M. T. Sulthana, Veerachamy Alagarsamy, and V. Raja Solomon
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Anti-Inflammatory Agents ,Histamine Antagonists ,Computational biology ,01 natural sciences ,chemistry.chemical_compound ,Structure-Activity Relationship ,Anti-Infective Agents ,Drug Discovery ,Quinazoline ,Structure–activity relationship ,Animals ,Humans ,Hypnotics and Sedatives ,Antihypertensive Agents ,Pharmacology ,Quinazoline derivatives ,Analgesics ,010405 organic chemistry ,Mechanism (biology) ,Chemistry ,Drug discovery ,Organic Chemistry ,General Medicine ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Quinazolines ,Anticonvulsants - Abstract
Most of the drugs and pharmacologically relevant molecules possess heterocyclic ring structures and presence of hetero atoms or groupings divulges privileged specificities in their pharmacological targets. Especially the heterocyclic systems, quinazoline is a biologically imperative scaffold known to be linked with several pharmacological activities. Some of the protuberant pharmacological responses attributed to this system are analgesic, anti-inflammatory, anti-convulsant, sedative-hypnotic, anti-histaminic, anti-hypertensive, anti-cancer, anti-microbial, anti-tubercular and anti-viral activities. This multiplicity in the pharmacological response contours of quinazoline has attracted the consideration of medicinal chemists to explore this system to its multiple potential against numerous activities. Several of these synthetic and pharmacological investigations have been successively studied for structure-activity relationship (SAR) to correlate the particular structural features for their pharmacological target. The emerging understanding of quinazoline derivatives on their pharmacological target offer opportunities for novel therapeutics. This review principally emphases on the medicinal chemistry aspects including drug design, structure–activity relationships (SARs), and mechanism of actions of quinazoline derivatives. This review gives detailed attention on in vitro and in vivo pharmacological activities of quinazoline and its analogs in the perspective of drug discovery and its development. more...
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- 2017
37. Microwave-assisted synthesis, characterization and biological activity of novel pyrazole derivatives
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Govindaraj Saravanan, Chinnasamy Rajaram Prakash, Palanirajan Vijayaraj Kumar, and Theivendren Panneer Selvam
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Analgesic activity ,Toxicity data ,Chemistry(all) ,Analgesic ,Biological activity ,General Chemistry ,Diclofenac Sodium ,Pyrazole ,Combinatorial chemistry ,Microwave assisted ,lcsh:Chemistry ,Anti-inflammatory activity ,chemistry.chemical_compound ,lcsh:QD1-999 ,chemistry ,Reagent ,Organic chemistry ,GeneralLiterature_REFERENCE(e.g.,dictionaries,encyclopedias,glossaries) ,ComputingMilieux_MISCELLANEOUS - Abstract
A series of 1-(4-substitutedphenyl)-3-phenyl-1 H -pyrazole-4-carbaldehydes 4a–l have been synthesized and tested for their biological activities. Formation of the pyrazole derivatives was achieved by treating with Vilsmeier-Haack reagent. The newly synthesized compounds were evaluated for their anti-inflammatory and analgesic activities compared to Diclofenac sodium as standard drug. Compounds 4g , 4i and 4k exhibited the maximum anti-inflammatory and analgesic activities. The detailed synthesis, spectroscopic and toxicity data are reported. more...
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- 2014
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38. Synthesis and pharmacological investigations of novel 2-phenylquinazolin-4(3H)-one derivatives
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Pandurangan Dinesh Kumar, Veerachamy Alagarsamy, and Govindaraj Saravanan
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Trifluoromethyl ,Organic Chemistry ,Biological activity ,Ulcer index ,Antimicrobial ,chemistry.chemical_compound ,chemistry ,Anthranilic acid ,Proton NMR ,Quinazoline ,Organic chemistry ,General Pharmacology, Toxicology and Pharmaceutics ,Isoxazole ,Nuclear chemistry - Abstract
A series of novel 2-phenyl-3-(4-(5-substitutedphenylisoxazol-3-yl)phenyl)quinazolin-4(3H)-one 5a–5o were designed and synthesized from anthranilic acid. All the synthesized compounds were characterized by FT-IR, 1H NMR, mass spectroscopy, and bases of elemental analysis. Tail-flick technique, carrageenan-induced foot paw edema test, and agar streak dilution test were performed for screening analgesic, anti-inflammatory and in vitro antimicrobial activity, respectively. Moreover, all compounds were examined for its ulcerogenicity. Results of biological studies revealed that all title compounds exhibited mild to good analgesic, anti-inflammatory, and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds was discussed. Out of fifteen title compounds, 2-phenyl-3-(4-(5-(4-(trifluoromethyl)phenyl)isoxazol-3-yl)phenyl) quinazolin-4(3H)-one 5f was found to be the most active compound. more...
- Published
- 2014
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39. Synthesis, characterization and antimicrobial activity of some novel benzimidazole derivatives
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Jarugula Udaya Bhavana, Janga Vamsi, Govindaraj Saravanan, Pamidipamula Supriya, Mittineni Venkata Sunil Kumar, and Immadisetty Sri Krishnanjaneyulu
- Subjects
Benzimidazole ,Chalcone ,mannich base ,Trifluoromethyl ,food.ingredient ,lcsh:RM1-950 ,chalcone ,lcsh:RS1-441 ,Mannich base ,Pyrazole ,Antimicrobial ,Antibacterial ,pyrazole ,lcsh:Pharmacy and materia medica ,chemistry.chemical_compound ,food ,lcsh:Therapeutics. Pharmacology ,chemistry ,Organic chemistry ,Agar ,Original Article ,Sodium acetate ,antifungal - Abstract
A series of novel N-((1H-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-substituted-4, 5-dihydro-1-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-substituted-4, 5-dihydro-1H-pyrazol-3-yl) benzenamine were synthesized by treating various 1-(4-((1H-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one with phenyl hydrazine in the presence of sodium acetate through a simple ring closure reaction. The starting material, 1-(4-((1H-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one,-benzoimidazol-1-yl) methylamino) phenyl)-3-substitutedprop-2-en-1-one, was synthesized from o-phenylenediamine by a multistep synthesis. All the synthesized compounds were characterized by spectroscopic means and elemental analyses. The title compounds were investigated for in vitro antibacterial and antifungal properties against some human pathogenic microorganisms by employing the agar streak dilution method using Ciprofloxacin and Ketoconazole as standard drugs. All title compounds showed activity against the entire strains of microorganism. Structural activity relationship studies reveal that compounds possessing an electron-withdrawing group display better activity than the compounds containing electron-donating groups, whereas the unsubstituted derivatives display moderate activity. Based on the results obtained, N-((1H-benzoimidazol-1-yl) methyl)-4-(1-phenyl-5-(4-(trifluoromethyl) phenyl)-4,5-dihydro-1H-pyrazol-3-yl) benzenamine 5i was found to be very active compared with the rest of the compounds and standard drugs that were subjected to antimicrobial assay. more...
- Published
- 2014
40. Assessment of prescribing pattern, adverse drug reactions and psychological distress in cancer patients at Erode Cancer Centre.
- Author
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SUKUMARAN, BHAVATHARINI, JAMES, JINCY, KANDASAMY, KRISHNAVENI, RAMANATHAN, SAMBATHKUMAR, GOVINDARAJ, SARAVANAN, and KANDAPPAN, VELAVAN
- Subjects
DRUG side effects ,PSYCHOLOGICAL distress ,MEDICAL personnel ,PSILOCYBIN ,DRUG prescribing ,DULOXETINE ,DRUG utilization - Abstract
Context: Cancer is a complex neoplastic disorder. Globally, it is said to be the second leading cause of death. Aim: The aim of the present study was to assess the prescribing pattern, adverse drug reactions, potential drug-drug interactions and psychological distress in cancer patients. Settings and Design: A prospective observational study was carried out on 65 cancer patients for 6 months at Erode Cancer Centre. Methods and Material: A socio-demographic questionnaire, Naranjo's and Hartwig's scales to evaluate the probability and severity of adverse drug reactions and Depression, Anxiety and Stress Scale 21 for psychological distress were used. Potential Drug-Drug Interactions were examined by Micromedex®. Statistical analysis used: Descriptive analysis was performed and outcomes were presented in percentage. Results: Most of the study participants had carcinoma cervix 10(15.3%). The most frequently prescribed anticancer drug was cisplatin 48(73.8%). Cyclophosphamide + doxorubicin 6(46.1%) was found mostly of the 13 PDDIs identified. ADRs were commonly experienced with mucositis 18(25%), alopecia 11(15.2%) and vomiting 10(13.8%). 63(87.5%) were probable ADRs and 54(75%) were found to be moderate in severity. The overall psychological distress showed 70.7% depression, 77% anxiety and 66.1% stress. Conclusion: To prevent morbidity and mortality among cancer patients, due consideration should be provided to monitor the rational use of drugs. Proper screening of PDDIs and spontaneous reporting of ADRs can be emphasized by health care professionals with psychosocial care. [ABSTRACT FROM AUTHOR] more...
- Published
- 2020
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41. A Comparitive Study on Road Traffic Accident in Kerala and Tamil Nadu: A Secondary Data Analysis.
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Abinaya, N. Venkata and Govindaraj, Saravanan
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TRAFFIC accidents ,SECONDARY analysis ,MOTOR vehicles ,NATION-state - Abstract
Background: Injuries are neglected significant public health problem worldwide which; requires organized efforts for prevention. The vehicle population of India constitutes only 1 percent of the world but accounts for nearly 10% of the total accidents in the world. Globalization has led to increased vehicular movements leading to unsafe roads. Materials and Method: This study aims at providing, comparison between Tamil Nadu and Kerala on the basis of Injury rates, on type of vehicle involved, type of roads and causative factor leading to road traffic crashes. In order to understand the severity of accidents and trends over time, we have collected data from various state and national reports published on various forums regarding the accidents in India, Tamil Nadu and Kerala and analyzed the data to see the trends and number of injuries over the past 3 years. Results: Between the two states, Tamil Nadu has shown high injury rates comparatively to Kerala over the period of 3 years. Though there are measures in place, somewhere there is a lack in proactive measure to stop this modern epidemic of motor vehicle trauma which shows an increase in accidents in Tamil Nadu than in Kerala. [ABSTRACT FROM AUTHOR] more...
- Published
- 2020
42. Synthesis, analgesic, anti-inflammatory and in vitro antimicrobial activities of some novel isoxazole coupled quinazolin-4(3H)-one derivatives
- Author
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Veerachamy Alagarsamy, Govindaraj Saravanan, and Pandurangan Dineshkumar
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Male ,Stereochemistry ,medicine.drug_class ,Analgesic ,Anti-Inflammatory Agents ,Ulcer index ,Anti-inflammatory ,Mice ,Structure-Activity Relationship ,chemistry.chemical_compound ,Anti-Infective Agents ,Toxicity Tests ,Drug Discovery ,medicine ,Animals ,Rats, Wistar ,Isoxazole ,Quinazolinones ,Analgesics ,Trifluoromethyl ,Chemistry ,Organic Chemistry ,Biological activity ,Isoxazoles ,Antimicrobial ,In vitro ,Rats ,Disease Models, Animal ,Molecular Medicine ,Female - Abstract
A series of novel isoxazole coupled quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, 1H NMR, mass spectroscopy and bases of elemental analysis with the aim of developing potent analgesic, anti-inflammatory and antimicrobial agents. Tail-flick technique, carrageenan-induced foot paw edema test and agar streak dilution test were performed for screening analgesic, anti-inflammatory and in vitro antimicrobial activity respectively. Moreover all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to good analgesic, anti-inflammatory and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds was discussed. Out of various synthesized compounds, 2-methyl-3-(4-(5-(4-(trifluoromethyl)phenyl) isoxazol-3-yl)phenyl)quinazolin-4(3H)-one 5e was found to be the most active compound. more...
- Published
- 2013
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43. Synthesis and anticonvulsant activity of novel quinazolin-4(3H)-one derived pyrazole analogs
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Veerachamy Alagarsamy and Govindaraj Saravanan
- Subjects
Phenytoin ,Stereochemistry ,medicine.medical_treatment ,Organic Chemistry ,Pharmacology toxicology ,Neurotoxicity ,Pyrazole ,medicine.disease ,chemistry.chemical_compound ,Anticonvulsant ,chemistry ,medicine ,Oral route ,General Pharmacology, Toxicology and Pharmaceutics ,medicine.drug - Abstract
Eighteen novel 6,8-(dibromo/unsubstituted)-2-(methyl/phenyl)-3-(4-(5-(substitutedphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carbonyl)phenyl)-quinazolin-4(3H)-ones 4a–4r were designed and synthesized in good yield. Antiepileptic screening of the title compounds was performed using MES and scPTZ seizures tests while the neurotoxicity was determined by rotorod test. In the preliminary screening, compounds 4d, 4e, 4p, 4q, and 4r were found active in MES model, while 4a, 4d, 4f, 4m, and 4p showed significant antiepileptic activity in scPTZ model. Further, all these eight compounds were administered to rats and compounds 4e, 4p, and 4q showed better activity than Phenytoin in oral route. Among these compounds 4p revealed protection in MES after i.p. administration at a dose of 30 mg/kg (0.5 h) and 100 mg/kg (4 h). The compound 4p also provided protection in the scPTZ at a dose of 100 mg/kg (0.5 h) and 300 mg/kg (4 h). more...
- Published
- 2012
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44. Anticonvulsant Activity of Novel 1-(Substituted Benzylidene)-4-(1-(Morpholino/Piperidino Methyl)-2,3-Dioxoindolin-5-yl) Semicarbazide Derivatives in Mice and Rats Acute Seizure Models
- Author
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Chinnasamy Rajaram Prakash, S. Raja, and Govindaraj Saravanan
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Pharmacology ,Phenytoin ,Semicarbazide ,Morpholino ,Semicarbazides ,Chemistry ,medicine.medical_treatment ,Isatin ,Organic Chemistry ,Neurotoxicity ,medicine.disease ,Biochemistry ,chemistry.chemical_compound ,Anticonvulsant ,In vivo ,Drug Discovery ,medicine ,Molecular Medicine ,medicine.drug - Abstract
A series of novel 1-(substituted benzylidene)-4-(1-(morpholino/piperidino methyl)-2,3-dioxoindolin-5-yl) semicarbazides 6a–6t was designed and synthesized on the basis of semicarbazide-based pharmacophoric model to meet the structural requirements necessary for anticonvulsant activity. The compounds were subjected to in vivo antiepileptic evaluation using maximal electroshock test and subcutaneous pentylenetetrazole seizure test methods. The neurotoxicity was determined by rotorod test. In the preliminary screening, compounds 6c, 6d, 6g, 6h, and 6m were found active in maximal electroshock test model, while 6g, 6i, 6m, and 6o showed significant antiepileptic activity in subcutaneous pentylenetetrazole seizure test model. Further, the compounds 6c, 6d, 6g, 6h, 6i, and 6m were administered orally to rats, of which 6c and 6g showed better activity than phenytoin. Among the synthesized compounds, 6g revealed excellent protection in both models with lower neurotoxicity. more...
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- 2012
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45. Design and synthesis of 4-(1-(4-chlorobenzyl)-2,3-dioxoindolin-5-yl)-1-(4-substituted/unsubstituted benzylidene) semicarbazide: Novel agents with analgesic, anti-inflammatory and ulcerogenic properties
- Author
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Govindaraj Saravanan, Chinnasamy Rajaram Prakash, and S. Raja
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Semicarbazide ,Schiff base ,medicine.drug_class ,Isatin ,Analgesic ,General Chemistry ,Ulcer index ,Medicinal chemistry ,Anti-inflammatory ,chemistry.chemical_compound ,chemistry ,Novel agents ,medicine ,Organic chemistry ,Paw edema - Abstract
A new series of isatin semicarbazide derivatives ( 7a – 7j ) were synthesized and characterized by spectroscopic means and elemental analysis. Analgesic and anti-inflammatory screening was performed using tail-flick technique and the carrageenan-induced foot paw edema test respectively. The ulcerogenicity was also determined for all the compounds. Some of the compounds showed moderate enhancement of the activity. Among the synthesized derivatives, compound 7d showed higher analgesic, antiinflammatory and one-third of ulcer index of the reference drug. more...
- Published
- 2012
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46. Design, synthesis and anticonvulsant activities of novel 1-(substituted/unsubstituted benzylidene)-4-(4-(6,8-dibromo-2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)phenyl) semicarbazide derivatives
- Author
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Govindaraj Saravanan, Chinnasamy Rajaram Prakash, and Veerachamy Alagarsamy
- Subjects
Phenytoin ,Stereochemistry ,medicine.medical_treatment ,Clinical Biochemistry ,Pharmaceutical Science ,Biochemistry ,Structure-Activity Relationship ,chemistry.chemical_compound ,Seizures ,Drug Discovery ,medicine ,Oral route ,Animals ,Structure–activity relationship ,Molecular Biology ,Quinazolinone ,Quinazolinones ,Semicarbazide ,Schiff base ,Dose-Response Relationship, Drug ,Organic Chemistry ,Rats ,Semicarbazides ,Anticonvulsant ,chemistry ,Design synthesis ,Drug Design ,Molecular Medicine ,Anticonvulsants ,Neurotoxicity Syndromes ,medicine.drug - Abstract
Novel quinazolinone derivatives 5a-5n were designed, synthesized and screened for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by rotorod test. Compounds 5c, 5d, 5g, 5j and 5k were found active in the preliminary screening in MES model and/or scPTZ model. Further all these five compounds were administered to rats, 5c and 5d showed better activity than Phenytoin in oral route. Among all the title compounds tested, the most active one was 5c that revealed protection in MES at a dose of 30 mg/kg (ip) after 0.5 and 4h. This molecule also provided protection in the scPTZ at a dose of 100mg/kg (0.5h) and 300 mg/kg (4h). more...
- Published
- 2012
- Full Text
- View/download PDF
47. Synthesis, analgesic, anti-inflammatory, and in vitro antimicrobial activities of some novel quinazolin-4(3H)-one derivatives
- Author
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Govindaraj Saravanan, Chinnasamy Rajaram Prakash, and Veerachamy Alagarsamy
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Trifluoromethyl ,medicine.drug_class ,Organic Chemistry ,Analgesic ,Biological activity ,Pharmacology ,Ulcer index ,Antimicrobial ,Anti-inflammatory ,In vitro ,chemistry.chemical_compound ,chemistry ,medicine ,General Pharmacology, Toxicology and Pharmaceutics ,Acetamide - Abstract
With the aim of developing potent analgesic, anti-inflammatory, and antimicrobial agents a series of novel quinazolin-4(3H)-one derivatives were synthesized and characterized by FT-IR, 1H-NMR, mass spectroscopy and bases of elemental analysis. Tail-flick technique, carrageenan-induced foot paw edema test, and agar streak dilution test were performed for screening analgesic, anti-inflammatory, and in vitro antimicrobial activity, respectively. Moreover, all compounds were examined for its ulcerogenicity. Results revealed that entire series of compounds exhibited mild to good analgesic, anti-inflammatory, and antimicrobial activity with low to moderate ulcer index. The relationship between the functional group variation and the biological activity of the evaluated compounds were discussed. Compound 2-(2-(4-(trifluoromethyl)benzylidene)hydrazinyl)-N-(4-(2-methyl-4-oxoquinazolin-3(4H)-yl) phenyl) acetamide 5e was determined to be the most active compound. more...
- Published
- 2012
- Full Text
- View/download PDF
48. Synthesis and anti-microbial screening of novel schiff bases of 3-amino-2-methyl quinazolin 4-(3H)-one
- Author
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Chinnasamy Rajaram Prakash, Perumal Pannerselvam, and Govindaraj Saravanan
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anti-fungal ,3-amino-2-methyl quinazolin-4-(3H)-one ,Schiff base ,biology ,Stereochemistry ,lcsh:RM1-950 ,Aspergillus niger ,Bacillus cereus ,lcsh:RS1-441 ,Pharmaceutical Science ,biology.organism_classification ,medicine.disease_cause ,Aspergillus fumigatus ,lcsh:Pharmacy and materia medica ,chemistry.chemical_compound ,lcsh:Therapeutics. Pharmacology ,chemistry ,Staphylococcus epidermidis ,anti-bacterial ,Anthranilic acid ,medicine ,Original Article ,Micrococcus luteus ,Escherichia coli - Abstract
In the present study, novel Schiff bases were synthesized by condensation of 3-amino-2-methyl quinazolin-4-(3H)-ones with different aromatic aldehydes. The 3-amino-2-methyl quinazolin-4-(3H)-one was synthesized from anthranilic acid via the 2-methyl benzoxazin-4-one. The chemical structures of the synthesized compounds were confirmed by means of Infrared (IR), (1)H-NMR, (13)C-NMR, Mass spectral, and Elemental analysis. These compounds were screened for anti-bacterial (Staphylococcus aureus ATCC 9144, Staphylococcus epidermidis ATCC 155, Micrococcus luteus ATCC 4698, Bacillus cereus ATCC 11778, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 2853, and Klebsiella pneumoniae ATCC 11298)) and anti-fungal (Aspergillus niger ATCC 9029 and Aspergillus fumigatus ATCC 46645) activities, using the paper disk diffusion technique. The minimum inhibitory concentrations (MIC) of the compounds were also determined by the agar streak dilution method. Most of the synthesized compounds exhibited significant anti-bacterial and anti-fungal activities. Among the synthesized compounds, 3-(4-hydroxy benzylideneamino)-2-methyl quinazolin-4(3H)-one 4g and 4c was found to exhibit the highest anti-bacterial activity and 3-(4-hydroxy-3-methoxy benzylideneamino)-2-methyl quinazolin-4(3H)-one 4k exhibited the highest anti-fungal activity. more...
- Published
- 2010
49. Synthesis and pharmacological investigation of novel 4-(4-Ethyl phenyl)-1-substituted-4H-[1,2,4]triazolo[4,3-a]-quinazolin-5-ones as new class of H1-antihistaminic agents
- Author
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Sankaranarayanan Murugesan, Govindaraj Saravanan, P. Parthiban, Veerachamy Alagarsamy, K. Dhanabal, V. Raja Solomon, and G. V. Anjana
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Chemistry ,Organic Chemistry ,Organic chemistry - Published
- 2008
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50. LC Method for the Determination of the Stability of Levetiracetam Drug Substance under Stressing Conditions
- Author
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G. Jyothi, M. Ramakrishna, B. Ravibabu, Govindaraj Saravanan, A. Annerao, Y. Suresh, and M. Yogeshwar Reddy
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Drug ,Chromatography ,Chemistry ,media_common.quotation_subject ,Organic Chemistry ,Clinical Biochemistry ,Biochemistry ,High-performance liquid chromatography ,Analytical Chemistry ,Hydrolysis ,chemistry.chemical_compound ,Forced degradation ,medicine ,Acid hydrolysis ,Levetiracetam ,Quantitative analysis (chemistry) ,Phosphoric acid ,medicine.drug ,media_common - Abstract
Levetiracetam is used in combination with other medications to treat certain types of seizures in people with epilepsy. Levetiracetam is in a class of medications called anticonvulsants and it works by decreasing abnormal excitement in the brain. A chromatographic separation was achieved on a YMC pack ODS AQ, 250 mm × 4.6 mm, 5 μm column using diluted phosphoric acid and acetonitrile in the ratio 85:15 v/v. Forced degradation studies were performed on the levetiracetam drug substance. The drug substance was degraded to Imp-B during acid and base hydrolysis. When the stress samples were assayed, the mass balance was matching. The sample solution and mobile phase was found to be stable up to 48 h at 25 °C. The developed method was validated with respect to linearity, accuracy, precision and robustness. more...
- Published
- 2007
- Full Text
- View/download PDF
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