Studies on Thiazole Derivatives. IV

Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase Inhibitors.

A series of novel isatin-thiazole derivatives were synthesized and screened for their in vitro α-glucosidase inhibitory activity. These compounds displayed a varying degree of α-glucosidase inhibitory activity with IC50 ranging from 5.36 ± 0.13 to 35.76 ± 0.31 μm as compared to the standard drug acarbose (IC50 = 817.38 ± 6.27 μm). Among the series, compound 6p bearing a hydroxyl group at the 4-...

Synthesis of New Thiazole, Bithiazolidinone and Pyrano[2,3-d ]thiazole Derivatives as Potential Antimicrobial Agents

In an attempt to find a new class of antimicrobial agents, a series of thiazole derivatives containing furan moiety 3, 7, 8a,b, 10a-c and 12 were prepared via the reaction of 2-cyano-N-(furan-2-ylmethyl)acetamide (1) with phenyl isothiocyanate and α-halocarbonyl compounds. Also, many bithiazolidinone and pyranothiazole derivatives were synthesized through interaction of thiazolidinone 7 with ap...

Studies on nicotinamide derivatives.

Synthesis, characterization and antimicrobial screening of novel quinoline-thiazole derivatives

2-Chloroquinoline-3-carbaldehyde 1 reacts with 2-cyanoacetohydrazide in ethanol to result in 1-[1-aza-2-(2-chloro(3quinolyl))vinyl]-2-cyanoacetamide 2. Phenyl isothiocyanate added to a stirred solution of compound 2, sulphur and triethylamine in a mixed solvent of dimethylformamide : ethanol to result in N-[1-aza-2-(2-chloro(3-quinolyl))vinyl](4amino-3-phenyl-2-thioxo(1,3-thiazoline-5-yl)) carb...

Fused Thiopyrano[2,3-d]thiazole Derivatives as Potential Anticancer Agents

rel-(5aR,11bR)-3,5a,6,11b-tetrahydro-2H,5H-chromeno[4',3':4,5]thiopyrano[2,3-d][1,3]thiazol-2-ones formed by the stereoselective Knoevenagel-hetero-Diels-Alder reaction were functionalized at the nitrogen in position 3 via reactions of alkylation, cyanoethylation, and acylation. The synthesized compounds were evaluated for their anticancer activity in NCI60 cell lines. Among the tested compound...