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A novel series of imidazole appended quinoline derivatives (6a–j) have been synthesized using the one-pot three-component reaction that occurred between the starting materials of substituted 2-phenoxyquinolin-3-carbaldehydes (3a-j), benzil (4), and ammonium acetate (5) by taking equimolar ratio. The newly synthesized imidazole-appended quinolines were subjected to probable inhibition against the anti-diabetic drug target maltase enzyme. The efficacy was tested using in-silico molecular docking analysis and molecular dynamics simulation. The studies revealed that the test 6f ligand (3-(4,5-diphenyl-1H-imidazol-2-yl)-2-phenoxy quinoline) is a strong inhibitor of the target protein maltase when compared with the known inhibitor acarbose and sheds new light on the medicinal chemistry research for the application of the synthesized 6f ligand in the pharmaceutical industry. [ABSTRACT FROM AUTHOR]

An efficient synthesis of new 4-hydroxy-3-(6-aryl-2-(arylamino) pyrimidin-4-yl) quinolin-2(1H)-ones 5a–j, 6a–j, and the evaluation of their antimicrobial activity have been described. Potent antibacterial activity was shown by 6a, 5e, 5f, 6h, 6i, 5j against the testes pathogenic bacteria. Also significant antifungal activity was shown by 6b, 6d, 5e toward selective fungal strains. [ABSTRACT FROM AUTHOR]

A new series of 6-oxo-1,6-dihydropyrimidin-5-carboxamides (4a–m) has been synthesized and reported with good yields. All these compounds were characterized using various spectral techniques such as IR, 1H NMR, 13C NMR, and HRMS and then subjected to in-vitro anti-oxidant and anti-bacterial activities using DPPH and microdilution methods, respectively. Among the synthesized pyrimidine-5-carboxamides, compounds 4a–b, 4j, and 4i were found to exhibit promising antibacterial activity compared to the standard drug Neomycin. Similarly, compounds 4g–i and 4l displayed excellent anti-oxidant activities against the standard drug ascorbic acid. [ABSTRACT FROM AUTHOR]

A new series of bi, tri-podal quinoline derivatives were synthesized by treating substituted phenols of (2-phenoxyquinolin-3-yl)methanols (5a–j) with the brominating reagents such as 1,2-bis(bromomethyl)benzene (6) and 1,3,5-tris(bromomethyl)-2,4,6-trimethylbenzene (8) in the presence of NaH as a base, afforded bi-podal (7a–j) and tri-podal (9a–j) quinoline derivatives respectively. All the newly synthesized compounds (7a–j and 9a–j) were found to be obtained with good yield in lesser time. Generally, single quinoline core moiety possessing molecules are biologically active and were displayed wide range of applications in medicinal field, but here we have synthesized molecules with two, three quinoline moiety, and expect that definitely they may play a greater role in medicinal activities compared with single quinoline possessed molecules and all the newly synthesized bi, tri-podal molecules were subjected to molecular docking studies with alpha-amylase and alpha-glucosidase enzymes to envisage the binding efficacy with comparative studies of standard drug acarbose. [ABSTRACT FROM AUTHOR]

An efficient multi component reaction for the synthesis of new 3‐(2‐amino‐6‐arylpyrimidin‐4‐yl)‐4‐hydroxyquinolin‐2(1H)‐ones has been described. Synthesized derivatives were screened for their in vitro antimicrobial and 2, 2‐diphenyl‐1‐picrylhydrazyl (DPPH) scavenging activity. Among the tested compounds 3 k, 3 m and 3 r shown better antibacterial properties and have displayed broad spectrum of activity than Neomycin against Staphylococcus aureus, Bacillus cereus, Klebsiella planticola, Escherechia coli, S.aureus and Pseudomonas aeruginosa. Moreover 3 r, 3 t and 3 n were found to have potent antifungal activity against Candida parapsilosis, Candida albicans, Aspergillus niger, Candida glabrata, Issatchenkia hanoiensis and Candida than the standard Miconazole. Furthermore 3 c, 3 j, 3 d, 3 m, and 3 h showed strong DPPH free radical scavenging activity than Ascorbic acid. [ABSTRACT FROM AUTHOR]

An efficient thiocarbohydrazide based fluorescencesensor S5 for the selective detection of Hg2+ in semi‐aqueous medium has been successfully designed and synthesized. The absorption (UV‐Vis) and emission (fluorescence) properties of S5 were studied in various solvents. The sensor S5 displayed no distinct changes in absorption with various solvents; however some remarkable changes were noticed in fluorescence studies. Solvent dependent spectral characterization of S5 was explored via the Lippert‐Mataga plot. UV‐Vis and fluorescence studies also revealed that the sensor S5 could selectively detect Hg2+ ion over the other tested metal ions. The interaction of S5 with Hg2+ leads to colour change from colourless to yellow. The observed quenching in fluorescence intensity may be due to chelation enhanced fluorescence quenching (CHEQ). The sensing mechanism was arrived through DFT and 1H NMR titration studies. The limit of detection was found to be 1.26 nM with a wide pH range of 4–10. Moreover, sensor S5 could demonstrate sensing efficiency for lower concentrations of Hg2+ in real sample analysis. Its performance, as a test strip and in analysis of various water samples conferred its superior selectivity. [ABSTRACT FROM AUTHOR]

In this study, a pyrazole‐based (Py‐KS) chemosensor was successfully designed and synthesized via Knoevenagel condensation and utilized as a colorimetric chemosensor for selective determination of Hg2+ in semi‐aqueous media. The probe exhibits a typical absorption band at 519 nm upon interaction with Hg2+, which is responsible for remarkable color change from yellow to pink. The detection limit of Py‐KS for the analysis of Hg2+ was found to be 4.73×10−7 M. The binding modes of interaction of Py‐KS with Hg2+ have been determined by Job's plot which exhibits 2:1 (Py‐KS: Hg2+) ratio, and further confirmed with 1H NMR titration and FT‐IR analysis. The association constant of Py‐KS‐Hg2+ complex was found as 1.2×103 M−1 using Benesi‐Hildebrand method. The probe could be recyclable after appropriate treatment with the reagents such as EDTA. Moreover, the designed probe Py‐KS has successfully demonstrated for the detection of Hg2+ in real sample analysis. [ABSTRACT FROM AUTHOR]

Synthesis of 2‐amino‐6‐(1, 2‐dihydro‐4‐hydroxy‐2‐oxoquinolin‐3‐yl)‐4‐arylpyridine‐3‐carbonitrile has been accomplished via NbCl5 catalysed multicomponent reaction (MCR). The tested compounds showed better potency than Neomycin and a broad spectrum of antibacterial activity against Staphylococcus aureus, Bacillus cereus and Escherichia coli. Similarly some of these have showed good activity against Staphylococcus aureus, Klebsiella planticola and Escherichia coli that were comparable to Ciprofloxacin. Also these compounds possess good antifungal activity that was better than Miconazole and comparable to Ciprofloxacin hydrochloride. [ABSTRACT FROM AUTHOR]

Two diverged series of water‐soluble non‐peptidic quinoline analogues were designed and synthesized by sequential attachment of piperazine and various amino acids to quinoline scaffold at first and second position using peptide coupling procedures. All synthesized compounds were subjected to the in‐silico screening against HIV protease‐1 and the cytotoxicity property of all synthesized compounds was examined on HCT116 cells. The compound, which has threonine and piperazine in sequence at quinoline second position found to have significant HIV protease inhibition property and demonstrated cytotoxicity IC50 value at 22.7±0.59 nM. [ABSTRACT FROM AUTHOR]