Synthesis, in-Vitro Cytotoxicity and Antimicrobial Evaluations of Some Novel Thiazole Based Heterocycles
Heba Kamal Abd El-Mawgoud;
Abstract
Condensation of rhodanine (1) with pyrazol-3(2H)-one derivatives (2a–f) gave 5-substituted-2-thioxo-1,3-thiazolidin-4-one derivatives (3a–f). Reaction of compound (1) with 2-arylmethylidene-malononitrile (4a–d) yielded the unexpected derivatives (5a–d). The latter compounds were subjected to cyclization reactions with malononitrile under different basic conditions, hydroxylamine hydrochloride and/or thiourea to furnish the fused thiazole derivatives (6a–d) and (8–10a–d). Coupling of (1) with diazotized aromatic amines (11a–c) in pyridine afforded the arylhydrazones (12a–c). Fusion of latter compounds with malononitrile afforded the thiazolopyridazine derivatives (13a–c). The structures of the newly synthesized compounds were elucidated via spectral data and elemental analyses. The in-vitro cytotoxic activity of compounds (3a–f) against the cell line MCF-7 was evaluated. Also, the synthesized products were investigated for their antibacterial and antifungal activities against six standard organisms including the G bacteria, Staphylococcus aureus and Bacillus subtilis, G bacteria, Escherichia coli and Proteus vulgaris in addition to fungi, Candida albicans and Aspergillus flavus.
Other data
Title | Synthesis, in-Vitro Cytotoxicity and Antimicrobial Evaluations of Some Novel Thiazole Based Heterocycles | Authors | Heba Kamal Abd El-Mawgoud | Keywords | fused thiazole;cytotoxicity;antibacterial activity;antifungal activity | Issue Date | Dec-2019 | Publisher | © 2019 The Pharmaceutical Society of Japan | Journal | Chemical and Pharmaceutical Bulletin | Volume | 67 | Issue | 12 | Start page | 1314 | End page | 1323 | DOI | 10.1248/CPB.C19-00681 |
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