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We have developed novel series of 5-arylidene-1, 3-thiazolidin-4-one analogues using diethylamine as catalyst. Diethylamine was found suitable in synthesizing variety of title compounds in 62-85% yield. In-vitro anticancer activity of synthesized analogues was evaluated using human breast (MCF7), lung (Hop62) and hepatic (HepG2) cell lines using SRB assay. Amongst the synthesized compounds 9b, 9e, 9f are excellent in inhibiting growth of cancer cell lines with GI50 value <10µg/ml in comparison with Adriamycin standard. We have also performed docking studies using SHP2 in complex with inhibitor (PDB ID: 2Shp) but results were non-supportive, very weak. We found no correlation between anticancer studies and docking studies. [ABSTRACT FROM AUTHOR]

We recently identified two compounds of 5-benzylidene-2-phenylimino-1,3-thiazolidin-4-one (BPT) analog, 5-(4-methylbenzylidene)-2-phenylamino-1,3-thiazolidin-4-one (MMPT) and 5-(2,4-dihydroxybenzylidene)-2-phenylimino-1,3-thiazolidin-4-one (DBPT), that can effectively induce apoptosis in cancer cells but not in normal cells, independently of P-glycoprotein status. To further investigate the antitumor activity of BPT analogs, we obtained 18 commercially available analogs of BPT and synthesized 7 analogs in our lab, and analyzed their antitumor activity in various cancer cells, including paclitaxel- and vinorelbine-sensitive and -resistant human lung cancer cells. Two of the compounds were more potent than MMPT or DBPT in induction of apoptosis in certain cancer cell lines and remained tumor selective. Seven compounds did not induce any cytotoxic effects in any of the cell lines tested at the highest concentration tested (31 microM). The other compounds induced cytotoxic effects in some cancer cells but not in others or were less potent than MMPT and DBPT. Cell uptake studies showed that analogs that effectively induced cell killing in paclitaxel- and vinorelbine-resistant cells could be taken up easily by those cells despite their high levels of P-glycoprotein expression. These data further demonstrate that thiazolidinone analogs are not P-glycoprotein substrates and could be useful for treatment of P-glycoprotein overexpressing refractory cancers.

We newly synthesized organic selenium compounds (5-membered ring compounds) including 2-selenoxo-1,3-thiazolidin-4-ones (compounds A) and 3-alkoxy-4,5-dihydro-5-selenoxo-1H-1,2,4-triazole-1-carboxylates (compounds B). To address whether these compounds show antioxidative effects, we also examined their superoxide radical (O2−)-scavenging effects. Moreover, we examined the effects of compound Aa on the activation of mitogen-activated protein kinase/extracellular signal-regulated protein kinases (MAPK/ERK1/2) and suppression of hydrogen peroxide-induced cytotoxicity in rat pheochromocytoma cells (PC12 cells). We evaluated the O2−-scavenging activities of the compounds by a chemiluminescence method, and activation of ERK1/2 in PC12 cells was evaluated by Western blot analysis. At 166 μmol/L, the O2−-scavenging activities were markedly different among compounds A and B. 3-(2,6-Dimethylphenyl)-2-selenoxo-1,3-thiazolidin-4-one (compound Aa) exhibited the strongest superoxide anion-scavenging activity among compounds A and B. The concentration necessary for 50% inhibition of the activity (IC50) of compound Aa was 25.9 μmol/L. Compound Aa activated ERK1/2 of the PC12 cell, as did ebselen, and suppressed hydrogen peroxide-induced cytotoxicity more potently than ebselen. In addition, the toxicity of compound Aa was less than that of ebselen. From these results, it is assumed that compound Aa is a candidate drug to prevent oxidative stress-induced cell death. [ABSTRACT FROM PUBLISHER]

A new round of monkeypox virus has emerged in the United Kingdom since July 2022 and rapidly swept the world. Currently, despite numerous research groups are studying this virus and seeking effective treatments, the information on the open reading frame, inhibitors, and potential targets of monkeypox has not been updated in time, and the comprehension of monkeypox target ligand interactions remains a key challenge. Here, we first summarized and improved the open reading frame information of monkeypox, constructed the monkeypox inhibitor library and potential targets library by database research as well as literature search, combined with advanced protein modeling technologies (Sequence-based and AI algorithms-based homology modeling). In addition, we build monkeypox virus Docking Server, a web server to predict the binding mode between targets and substrate. The open reading frame information, monkeypox inhibitor library, and monkeypox potential targets library are used as the initial files for server docking, providing free interactive tools for predicting ligand interactions of monkeypox targets, potential drug screening, and potential targets search. In addition, the update of the three databases can also effectively promote the study of monkeypox drug inhibition mechanism and provide theoretical guidance for the development of drugs for monkeypox. [ABSTRACT FROM AUTHOR]

In this investigation, a novel series of quinoline analogues bearing thiazolidinones were designed and synthesized based on our previous study. Among them, the most potent compound 11k , 4-((4-(4-(3-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)ureido)phenoxy)-6-methoxyquinolin-7-yl)oxy)- N -isopropylpiperidine-1-carboxamide, possessed submicromolar c-Met and Ron inhibitory activities. In addition, enzymatic assays against a mini-panel of kinases (c-Kit, B-Raf, c-Src, IGF1R, PDGFRα and AXL) were performed, the results showed that compound 11k exhibited moderate inhibitory activity against PDGFRα, c-Src and AXL. MTT assay revealed in vitro antitumor activities against HT-29 cells of compound 11k with an IC 50 value of 0.31 μM which was 9.3- and 34.2-fold more potent than that of Regorafenib (IC 50 = 2.87 μM) and Cabozantinib (IC 50 = 10.6 μM). Preliminary antitumor mechanisms were also investigated by cellular assays. Considerable cytotoxicity, antiproliferation and induction of apoptosis of compound 11k in a dose- and time-dependent manner were confirmed by IncuCyte live-cell imaging assays. Treatment with compound 11k caused slight G2-or M-phase arrest in HT-29 cells. Further cell selectivity of compound 11k showed that it was not active against human normal colorectal mucosa epithelial cell FHC at 10.0 μg/mL. The above results support further structural modification of compound 11k to improve its inhibitory activity, which will lead to more potent anticancer agents. Image 1 • Novel quinoline analogues bearing thiazolidinones were designed and synthesized. • 11k possessing potent inhibitory activity against multi-kinases was identified. • Antitumor activity on HT-29 of 11k was 9.3-fold more potent than that of Regorafenib. • Excellent antiproliferation, cytotoxicity, and induction of apoptosis were confirmed. • The toxicity to FHC cells of 11k was much lower than that of Regorafenib. [ABSTRACT FROM AUTHOR]

The eccentric connectivity index, which has recently been employed successfully for the development of numerous mathematical models for the prediction of biological activities of diverse nature, has been reformed to overcome its limitations caused by degeneracy and insensitivity towards heteroatoms. The reformed eccentric connectivity index, termed the eccentric connectivity topochemical index, overcomes the limitations of the eccentric connectivity index by exhibiting very low degeneracy and displaying sensitivity to both the presence and relative position of heteroatoms without compromizing the discriminating power of the eccentric connectivity index. The relationship of the eccentric connectivity topochemical index, eccentric connectivity index and Wiener’s index with regard to the anti-HIV activity of 2, 3-diaryl-1, 3-thiazolidin-4-one derivatives was subsequently investigated. The values of the eccentric connectivity topochemical index, the eccentric connectivity index and Wiener’s index of each of 31 analogues comprizing the data set were computed using in-house computer program. Resultant data was analyzed and suitable models developed after identification of active ranges. Subsequently, each derivative was assigned a biological activity using these models, which was then compared with the reported anti-HIV activity. The accuracy of prediction using these models was found to vary from 81 to 90%. The proposed index offers a vast potential for virtual screening of combinatorial libraries, structure property/activity studies and drug design. Figure Basic structure of 2,3-diaryl-1, 3-thiazoidin-4-ones. [ABSTRACT FROM AUTHOR]

Viruses are a real threat to every organism at any stage of life leading to extensive infections and casualties. N-heterocycles can affect the viral life cycle at many points, including viral entrance into host cells, viral genome replication, and the production of novel viral species. Certain N-heterocycles can also stimulate the host's immune system, producing antiviral cytokines and chemokines that can stop the reproduction of viruses. This review focused on recent five- or six-membered synthetic N-heterocyclic molecules showing antiviral activity through SAR analyses. The review will assist in identifying robust scaffolds that might be utilized to create effective antiviral drugs with either no or few side effects. [ABSTRACT FROM AUTHOR]

The sonochemical synthesis, structural analysis, theoretical calculations, and the nonlinear optical (NLO) discovery of benzylidenehydrazono thiazolidin-4-one derivative 8, that is, (Z)-ethyl-2-((Z)-2-((E)-(4-chlorobenzylidene)hydrazono)-4-oxo-3-phenylthiazolidin-5-ylidene) acetate (C20H16ClN3O3S), are detailed. The 1H and 13C NMR data, melting point (m.p), infrared spectrum (IR), mass spectrum, and UV–visible spectrum measurements are used to confirm the authenticity of the synthesized derivative 8. The geometrical structural optimizations and theoretical properties of the synthesized compound are performed using density functional theory (DFT). The NLO properties of the synthesized derivative 8 are studied under continuous wave (cw) 473-nm laser beam via conducting the closed (C)- and open (O)-aperture (A) Z-scan techniques where the nonlinear refractive index (NLRI) and the nonlinear absorption coefficient (NLAC) are obtained, viz. 1.79 × 10−7 cm2/W and 2.72 × 10−3 cm/W, respectively, and an optical limiting (OLg) threshold of 13 mW is obtained. [ABSTRACT FROM AUTHOR]

A new and efficient method for the preparation of 2-(2-chloroquinolin-3-yl)-3-(4-methylphenyl)-1, 3-thiazolidin-4-one derivatives has been assembled by DCC:-mediated three-component one-pot reaction of amine, aldehyde, and mercaptoacetic acid. The final compounds were obtained in quantitative yields within 50 min. The synthesized compounds were characterized by elemental analysis, FT-IR, 1H-NMR, and mass spectral data. The selected compounds were studied for interaction with calf thymus DNA by electronic spectra, viscosity measurements as well as thermal denaturation studies. On binding to DNA, the absorption spectrum underwent bathochromic and hypochromic shifts. The binding constant (Kb) had a value of 5.3×105 M-1 for 2a and 5.8×105 M-1 for 3a. The viscosity measurements indicated that the viscosity of sonicated rod-like DNA fragments increased. [ABSTRACT FROM AUTHOR]

Thiazolidin‐4‐one is a versatile nucleus that has been reported to exhibit a diverse array of biological activities, including anticancer and antimicrobial activities. In the current research study, a series of C2‐(p‐substituted phenyl)‐thiazolidin‐4‐one compounds conjugated with anilines were designed and tested for drug‐likeness behaviour. Subsequently, the designed compounds were synthesized, characterized, and tested for anticancer activity against three cancer cell lines, namely liver (HEP−G2 cells), breast (MDA‐MB‐231), and glioblastoma (U87MG cells), with gemcitabine as the reference positive control drug. Initially, the compounds were tested at 50 micromolar, while the MIC was determined for the selected active compounds. Among the three cell lines, MDA‐MB‐231 showed relatively higher sensitivity towards the tested compounds. Four compounds of the series exhibited comparable or superior cytotoxicity to the reference drug gemcitabine. Particularly, N‐(p‐tolyl)‐2‐(2‐(4‐methoxyphenyl)‐4‐oxothiazolidin‐3‐yl)acetamide (6 d) displayed highest cytotoxicity among the series. The anticancer activity of the selected compounds was also tested against 3D spheroid models, in which compound N‐(4‐chlorophenyl)‐2‐(2‐(4‐methoxyphenyl)‐4‐oxothiazolidin‐3‐yl)acetamide (6 a) induced apoptosis in brain tumour spheroids (MTS). Docking studies of compound 6 d were performed against different targets, namely dihydrofolate reductase, phosphoinositide 3‐kinase, epidermal growth factor receptor, dihydroorotate dehydrogenase, and murine double minute 2, which illustrated inhibition of dihydroorotate dehydrogenase as a possible mechanism of toxicity. The compounds were also evaluated in vitro for antibacterial activity against two bacterial strains (E. coli and P. aeruginosa) and a Candida albicans fungal strain. [ABSTRACT FROM AUTHOR]

5-Acetyl-4-(4-methoxyphenyl)-6-methyl-2-thioxo-1,2-dihydropyridine-3-carbonitrile has been successfully prepared by the condensation between the acetylacetone and 2-cyano-3-(4'-methoxyphenyl)thio acrylamide and used to search for a potential drug that could be used to treat COVID-19. The structure was characterized and confirmed by X-ray diffraction analysis, and the crystal packing stability was also performed by the Hirshfeld surface analysis. The chemical reactivity and other properties of the title compound were determined using the density functional theory (DFT) computation and the NBO analysis. Also, the molecular electrostatic potential (MEP) surface was investigated. The CN group was the most nucleophilic site in the entire molecule based on the results. The title compound's in-silico molecular docking revealed a strong binding potential. Eventually, molecular dynamic (MD) simulation studies are conducted to examine the stability of the molecule inside the receptor cavity. The findings of the in-silico analysis manifested affirmative evidence for the title molecule with good binding, as a potent inhibitor for the main protease of SARS-Cov-2. Hence, it holds the striking potential to serve as a prospective lead compound for designing efficacious drugs against COVID-19. [ABSTRACT FROM AUTHOR]

The risk faced by the drug-resistant pathogens, research, and development for viable alternative medicine is gaining traction. This study aims to utilize agricultural waste beneficially, by investigating the methanol, ethanol, acetone, ethyl acetate, petroleum ether, and hexane extracts of black gram pods by gas chromatography-mass spectrometry (GC–MS), and Fourier transform infrared (FT-IR) analysis to identify metabolites and functional groups and to evaluate its antibacterial and anti-biofilm potential on various fish disease-causing drug resistant pathogens like Aeromonas hydrophila, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus. Numerous compounds were identified as major peak area percentage by GC–MS analysis based on the polarity. Methanolic and ethanolic extracts of black gram pods showed higher phenolic and tannin content compared to other solvents, these results correlate with antioxidant potential. IC50 values of both 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and ABTS (2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid)) by the methanolic extracts possessed 933.807 and 976.285 µg/mL respectively. All the extracts possessed potential antibiofilm activity against A. hydrophila, K. pneumoniae, P. aeruginosa, and S. aureus in a dose-dependent manner. This study clearly shows that phenolic content is the major source for the inhibition of bacterial cell adherence (biofilm) against pathogens. Extraction in highly polar solvents exhibited higher content of phenols and tannins as compared to non-polar solvents. Findings of the current study support black gram pods as an excellent alternative medicine against fish disease-causing pathogens. It is proved in this study that the biowaste black gram pods could be recycled for the welfare of humans as well as for the growth of the country's economy. [ABSTRACT FROM AUTHOR]

Cancer is one of the life-threatening diseases accountable for millions of demises globally. The inadequate effectiveness of the existing chemotherapy and its harmful effects has resulted in the necessity of developing innovative anticancer agents. Thiazolidin-4-one scaffold is among the most important chemical skeletons that illustrate anticancer activity. Thiazolidin-4-one derivatives have been the subject of extensive research and current scientific literature reveals that these compounds have shown significant anticancer activities. This manuscript is an earnest attempt to review novel thiazolidin-4-one derivatives demonstrating considerable potential as anticancer agents along with a brief discussion of medicinal chemistry-related aspects of these compounds and structural activity relationship studies in order to develop possible multi-target enzyme inhibitors. Most recently, various synthetic strategies have been developed by researchers to get various thiazolidin-4-one derivatives. In this review, the authors highlight the various synthetic, green, and nanomaterial-based synthesis routes of thiazolidin-4-ones as well as their role in anticancer activity by inhibition of various enzymes and cell lines. The detailed description of the existing modern standards in the field presented in this article may be interesting and beneficial to the scientists for further exploration of these heterocyclic compounds as possible anticancer agents. [ABSTRACT FROM AUTHOR]

Due to the lack of effective vaccine(s) against leishmania and also pharmacokinetics issues of current drugs, it is necessary to discover new antileishmanial agents. Within this particular study, a series of novel 1-aryl/alkyl-3-benzoyl/cyclopropanoyl thiourea derivatives were synthesized (yields 69–84%) and evaluated as antileishmanial compounds (1–11). Synthetic derivatives were subjected to in vitro antileishmanial assessment against Leishmania major promastigotes by colorimetric MTT assay. Compounds 3 (IC50 38.54 µg/mL), 5 (IC50 84.75 µg/mL) and 10 (IC50 70.31 µg/mL) exhibited higher activities after 48 h but were less potent than amphotericin B (IC50 0.19 µg/mL). Antileishmanial activities indicated priority of 5-methyl-4-phenyl thiazole over furyl methyl substituents and 4-phenyl thiazole on thiourea nitrogen. N-myristoyltransferase (NMT) was selected as a validated L. major target for molecular docking studies. In silico results indicated the contribution of hydrophobic, π-stacking and H-bond interactions in binding to target. Most of the synthesized derivatives had lower binding affinities to human NMT (hNMT) than leishmanial enzyme. Docking conformations of top-ranked selective binders (compounds 3 and 5) were subjected to 50 ns MD simulations inside L. major HMT (LmNMT) active site. MD trajectories were used to extract RMSD, RMSF, Rg and durability of intramolecular/intermolecular H-bonds of the complex. It was observed that compound 3 escaped from LmNMT binding site during simulation period and no stable complex could be envisaged. Unlike 3, compound 5 attained stable binding conformation with converged stability parameters. Although mechanistic details for antileishmanial effects of synthesized derivatives are to be explored, current results may be implicated in further structure-guided approach toward potent antileishmanial agents. [ABSTRACT FROM AUTHOR]

The preparation, characterization, and catalytic investigation of NiFe2O4@SiO2 grafted 3-(propyl azanediyl)bis(ethane-2,1-diyl) bis(hydrogen sulfate) nanoparticles (A) is described. The catalyst was characterized by FT-IR, XRD, FE-SEM, and DLS techniques. The main particle size by the DLS technique was determined as 52 nm. The catalyst was found to be efficient for the condensation of 9-methyl-9H-carbazol-3-amine, thioglycolic acid, and aldehydes lead to the formation of 3-(9-methyl-9H-carbazol-3-yl)-2-arylthiazolidin-4-one derivatives (1d-11d) under reflux in DMF DMF (Time: 1–2 h; Yields: 76–98%) and ultrasonic irradiation in DMF (Time: 0.8–1 h; Yields: 85–97%). The effect of solvent, temperature, and catalyst dosage on the reaction was studied. The catalyst can be recovered and reused 11 times. [ABSTRACT FROM AUTHOR]

Pesticides play an important role in crop disease and pest control. However, their irrational use leads to the emergence of drug resistance. Therefore, it is necessary to search for new pesticide-lead compounds with new structures. We designed and synthesized 33 novel pyrimidine derivatives containing sulfonate groups and evaluated their antibacterial and insecticidal activities. Results: Most of the synthesized compounds showed good antibacterial activity against Xanthomonas oryzae pv. Oryzae (Xoo), Xanthomonas axonopodis pv. Citri (Xac), Pseudomonas syringae pv. actinidiae (Psa) and Ralstonia solanacearum (Rs), and certain insecticidal activity. A5, A31 and A33 showed strong antibacterial activity against Xoo, with EC50 values of 4.24, 6.77 and 9.35 μg/mL, respectively. Compounds A1, A3, A5 and A33 showed remarkable activity against Xac (EC50 was 79.02, 82.28, 70.80 and 44.11 μg/mL, respectively). In addition, A5 could significantly improve the defense enzyme (superoxide dismutase, peroxidase, phenylalanine ammonia-lyase and catalase) activity of plants against pathogens and thus improve the disease resistance of plants. Moreover, a few compounds also showed good insecticidal activity against Plutella xylostella and Myzus persicae. The results of this study provide insight into the development of new broad-spectrum pesticides. [ABSTRACT FROM AUTHOR]

An unprecedented series of 2‐imino‐1,3‐thiazolidin‐4‐ones were designed by straightforward and dynamic technique via one‐pot three‐component reaction of isothiocyanatobenzene, primary amines, ethyl bromoacetate and/or phenacylbromide. Furthermore, we found that the reaction between 2‐imino‐1,3‐thiazolidin‐4‐one and arylidenemalononitrile using of C2H5ONa as catalyst gave the corresponding 3‐(2‐phenylethyl)‐5‐(4‐arylidene)‐2‐(phenyl imino)‐1,3‐thia‐zolidin‐4‐one instead of 5‐amino‐7‐aryl‐3‐(2‐phenylethyl)‐2‐(phenylimino)‐3,7‐dihydro‐2H‐6‐carbonitrile. The identical molecules were designed through other routes via the reaction of 2‐imino‐1,3‐thiazolidin‐4‐one with the corresponding aryl carbaldehyde. [ABSTRACT FROM AUTHOR]

In continuation of our previous work, a series of furan-thiazolidinone hybrids was prepared by Knoevenagel condensation of 3-(furan-2-ylmethyl)-2-(phenylimino)-1, 3-thiazolidin-4-one with different aryl aldehydes in presence of strong base. Some members of the series exhibited remarkable antiamoebic activity and cell viability. Three compounds (3 , 6 and 11) showed excellent binding energy for Entamoeba histolytica O -acetyle- l -serine sulfohydrolase and Entamoeba histolytica thioredoxin reductase. These compounds demonstrated significant inhibition of O -acetyle- l -serine sulfohydrolase. The promising antiamoebic activity and enzymatic assay of 3 , 6 and 11 make them promising molecules for further lead optimization in the development of novel antiamoebic agents. [ABSTRACT FROM AUTHOR]

Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Heterocycles possessing a pyrimidine scaffold have piqued tremendous interest of organic and medicinal chemists owing to their privileged bioactivities. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti‐inflammatory, antibacterial, and antihypertensive activities. This heterocycle, being a significant endogenous component of the body, the pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. The landscape of FDA approved drugs, presently marketed incorporating the pyrimidine scaffold continues to evolve in number and diversity. There is a tremendous surge in discovery of new targets across many diseases especially those involving emerging resistance to clinically used battery of drugs. Pyrimidine scaffolds will continue to be explored expanding their chemical space portfolio in an effort to find novel drugs impacting these targets. This review aims to provide an elaborate recapitulation of the recent trends adopted to synthesize propitious pyrimidine incorporated hits and also focuses on the clinical significance reported for functionalized pyrimidine analogues that would quintessentially aid medicinal chemists for new research explorations in this arena. [ABSTRACT FROM AUTHOR]

Oncological diseases have currently reached an epidemic scale, especially in industrialized countries. Such a situation has prompted complex studies in medicinal chemistry focused on the research and development of novel effective anticancer drugs. In this review, the data concerning new 4-thiazolidinone-bearing hybrid molecules with potential anticancer activity reported during the period from the years 2017–2022 are summarized. The main emphasis is on the application of molecular hybridization methodologies and strategies in the design of small molecules as anticancer agents. Based on the analyzed data, it was observed that the main directions in this field are the hybridization of scaffolds, the hybrid-pharmacophore approach, and the analogue-based drug design of 4-thiazolidinone cores with early approved drugs, natural compounds, and privileged heterocyclic scaffolds. The mentioned design approaches are effective tools/sources for the generation of hit/lead compounds with anticancer activity and will be relevant to future studies. [ABSTRACT FROM AUTHOR]

Hydrazones are active compounds having an azomethine –NHN=CH group and are widely studied owing to their ease of preparation and diverse pharmacological benefits. Novel isonicotinic hydrazone derivatives of vanillin aldehyde and salicyl aldehyde were synthesized that had azomethine linkages and were characterized by UV–Visible, FTIR, EI-MS, 1H-NMR and 13C-NMR spectroscopy. The compounds were screened for their antibacterial activity against Staphylococcus aureus, Bacillus subtilus, and Escherichia coli using disc diffusion and minimum inhibitory concentration (MIC) methods. For cytotoxicity, a brine shrimp lethality test was performed to calculate the lethal concentration (LC50). The results demonstrated appreciable antibacterial activities against the applied strains, amongst which the compounds coded NH3 and NH5 showed maximum inhibition and MIC responses. In terms of cytotoxic activity, the maximum effect was observed in compound NH5 and NH6 treatments with minimum survival percentages of 36.10 ± 3.45 and 32.44 ± 2.0, respectively. These hydrazones could be potential candidates in antitumorigenic therapy against various human cancer cells. [ABSTRACT FROM AUTHOR]

[Display omitted] • Novel phenyl-1,3-thiazolidin-4-one sulfonyl derivatives were synthesized anti-microbial and anti-viral activity. • Compounds 5d , 5f , 5g , 5h and 5j showed most potent antibacterial activity. • Compounds 5g , 5j , 5o , 5p and 5q showed good activity against fungal strains. • Compound 5h showed antiviral activity against HIV-1(strain IIIB) and HIV-2 (strain ROD). A series of novel substituted phenyl 1, 3-thiazolidin-4-one sulfonyl derivatives 5 (a-t) were synthesized and screened for their in-vitro anti-microbial and anti-viral activity. The result of the anti-microbial assay demonstrated compounds 5d, 5f, 5g, 5h, 5i, 5j showed prominent inhibitory activity against all the tested Gram-positive and Gram-negative bacterial strains, while compounds 5g, 5j, 5o, 5p, 5q showed significant activity against the entire set of fungal strains as compared to standard drug Ampicillin and Clotrimazole, respectively. The antimicrobial study revealed that compounds having electron-withdrawing groups showed significant antimicrobial potency. The most active antibacterial compound 5j showed potent inhibition of S. aureus DNA Gyrase enzyme as a possible mechanism of action for antimicrobial activity. Moreover, the antiviral testing of selected compounds showed considerable activity against Herpes simplex virus-1(KOS), Herpes simplex virus-2 (G), Herpes simplex virus-1(TK- KOS ACVr), Vaccinia virus, Human Coronavirus (229E), Reovirus-1, Sindbis virus, Coxsackie virus B4, Yellow Fever virus and Influenza A, B virus. Compounds 5h exhibited low anti-viral activity against HIV-1(strain IIIB) and HIV-2 (strain ROD). The study clearly outlined that synthesized compounds endowed with good antimicrobial property together with considerable antiviral activity. [ABSTRACT FROM AUTHOR]

In this review, we tried to underscore the synthesis of the heterocyclic compounds under assisted ultrasonic irradiation. The ultrasonic irradiation has been applied for medicinal chemistry and drug discovery process since it dramatically reduces reaction times, from days or hours to minutes. Also, ultrasonic irradiation provides lower cost, excellent yields, greater purity, and simple workups as compared to lower yields, longer reaction times, lesser purity and in the conventional methods. In this review, we have compared synthesis of the heterocyclic compounds under ultrasonic irradiation with other methods. [ABSTRACT FROM AUTHOR]

In this research, a highly efficient method is described for the synthesis of dihydropyrano[3,2-c]chromenes and biscoumarins using ionic liquids (ILs) supported on nano-FeNi3 as catalyst. The heterogeneous catalyst was fully characterized by X-ray diffraction (XRD), SEM, FT-IR, and vibrating sample magnetometer (VSM). [ABSTRACT FROM AUTHOR]

Background: The necessity for newer anti-HIV and anti-tubercular medications has arisen as a result of the prevalence of opportunistic infections caused by HIV (human immunodeficiency virus)., Objective: A series of ten new hydrazono 1,3-thiazolidin-4-one derivatives were synthesized in one-pot and evaluated for anti-HIV and anti-tubercular activities. Molecular Docking was accomplished with HIV-1 reverse transcriptase protein (PDB ID: 1REV) and Mycobacterium Tuberculosis (M. tuberculosis) H37Rv protein (PDB ID: 2YES) receptors along with drug-likeness and ADMET properties., Methods: One-pot synthesis of hydrazono 1,3-thiazolidin-4-one derivatives was carried out by ketones, thiosemicarbazide and ethylchloroacetate with the catalyst of anhydrous sodium acetate. All the synthesized compounds were characterized and evaluated for their in-vitro anti-HIV and also evaluated for their in-vitro anti-tubercular activity against M. tuberculosis H 37 Rv. In-silico predicted physicochemical parameters were done by MedChem DesignerTM software version 5.5 and ADMET parameters by pkCSM online tool. Furthermore, molecular docking was performed with pyrx 0.8 by autodock vina software., Results: All the synthesized compounds were characterized and evaluated for their in-vitro anti- HIV activity for inhibition of syncytia formation, which shows KTE1 with EC 50 47.95 μM and Selectivity Index (SI) of >4.17 and for inhibition of p24 antigen production EC 50 was found to be 80.02 μM and SI of >2.49. The compounds were also evaluated for their in-vitro anti-tubercular activity against M. tuberculosis H 37 Rv, in which KTE1 MIC values of 12.5μg/ml with SI of >4.0 and cytotoxicity against Vero cell lines. In-silico predicted physicochemical parameters for synthesized compounds which were found to be drug-like. Furthermore, docking has shown a good dock score and binding energy with anti-HIV and anti-tubercular receptors., Conclusion: From the novel synthesized molecules, none of the molecule is as effective as standards for anti-HIV and anti-tubercular drugs and hence can be further explored for its potential activities. Furthermore, derivatization was made to achieve more potent compounds for anti-HIV and anti-tubercular drugs., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

An efficient three-component synthesis of 1,3-thiazolidin-4-ones is described by one-pot condensation of aldehydes, aromatic amine and thioglycolic acid with nano-CoFe2O4@SiO2/PrNH2as a robust heterogeneous catalyst. The significant advantages of this protocol are the use of magnetically recoverable catalyst, high to excellent product yields, operational simplicity and the use of CoFe2O4@SiO2/PrNH2nanoparticles as an environment-friendly catalyst. [ABSTRACT FROM AUTHOR]

Ammonium persulfate can be used as a homogeneous catalyst for three-component one-pot synthesis of some 1,3-thiazolidin-4-one derivatives from aldehydes, amines and mercaptoacetic acid under solvent-free conditions with good yields. The characterization of products was generally achieved by IR and NMR techniques. Inexpensive catalyst, high yields, simple product isolation and high atom economy are the noteworthy aspects of the protocols. [ABSTRACT FROM AUTHOR]

Some novel 4-thiazolidinone derivatives have been synthesized by the condensation of isatin/5-chloroisatin with thiosemicarbazide to yield thiosemicarbazones, which were then cyclized to form corresponding thia-3,4,9-triaza-fluoren-2-ylamines. These were reacted with substituted aldehydes to give corresponding Schiff bases, which were cyclized using thioglycolic acid in the presence of zinc chloride to obtain the 4-thiazolidinone derivatives. All the synthesized compounds were characterized by spectral (IR, MS and NMR) and elemental analysis. The compounds were screened for their antibacterial activity against Gram-positive bacteria ( B. subtilis, S. aureus, B. pumilus and M. luteus), Gram-negative bacteria ( P. aeruginosa, E. coli and P. fluorescens) and for antifungal activity against A. niger and P. chrysogenum by agar-diffusion method. The minimum inhibitory concentrations of these compounds were also determined by tube dilution method. The antimicrobial effectiveness of all the compounds was found to be concentration dependent. Two compounds-2-methyl-3-(1-thia-3, 4, 9-triaza-fluoren-2-yl)-thiazolidin-4-one ( 7aI) and 2-naphthalen-1-yl-3-(1-thia-3, 4, 9-tri aza-fluoren-2-yl)-thiazolidin-4-one ( 7aII) -exhibited good antibacterial activity. The antibacterial activity of all the compounds was found to be better than the antifungal activity. [ABSTRACT FROM AUTHOR]