Thiazole-Based Thiazolidinones as Potent Antimicrobial Agents. Design, Synthesis and Biological Evaluation.

Thiazole-Based Thiazolidinones as Potent Antimicrobial Agents. Design, Synthesis and Biological Evaluation.
Comb Chem High Throughput Screen. 2015 Dec 2;
Authors: M H, C T, E T, A G
Abstract
As a part of our ongoing project on design and synthesis of new thiazole derivatives with antimicrobial activity fourteen new ethyl 2-(2-((E)-((Z)-5-(4-benzyliden)-4-oxothiazolidin-2-yliden)amino-4-yl)acetates , carrying halogens, methoxy and other groups were synthesized. Compounds were tested against eight Gram positive and negative bacteria as well as eight yeasts and mold by microdilution assay. All compounds showed good activity against all bacteria tested with MIC ranging between 2.3-39.8 μmol/ml x 10-2 and MBC of 9.2-79.6 μmol/ml x 10-2. As reference drugs Ampicillin (MIC 24.8-74.4 and MBC 37.2-124.0 μmol/ml x 10-2) and Streptomycin (MIC 4,3-17.2 and MBC 8.6-51.6 μmol/ml x 10-2) were used. The best activity was observed for 4-bromo derivative. All tested compounds showed excellent antifungal activity against all fungi tested with MIC in range between 0.3-38.6 μmol/ml x 10-2 and MFC range of 0.6-77.2 μmol/ml x 10-2, better than that of reference drugs, Ketoconazole (MIC 38.0-475.0 and MFC 95.0-570 μmol/ml x 10-2) and Bifonazole (MIC 48.0-64.0 and MFC 64.0-80.0 μmol/ml x 10-2). The best activity was observed for 3-nitro derivative. It was found that among the 5-arylidene derivatives the inhibitory effect appears to be dependent on th...

Source: Combinatorial Chemistry and High Throughput Screening - December 2, 2015 Category: Chemistry Authors: M H, C T, E T, A G Tags: Comb Chem High Throughput Screen Source Type: research