4-oxothiazolidine and 2-aminothiazole

Mycobacterium tuberculosis, which causes tuberculosis, continues to infect millions of the global population, resulting in 1.8 million deaths worldwide in 2015.. Hybrids of 2-amino-4-methylthiazole bearing 5-acetyl/5-ethyl carboxylate functionality with 5-arylidene thiazolidinone moiety (6a-k and 9a-d) were synthesized and screened for antitubercular and antimicrobial activities.. 5-ethyl carboxylate derivative 6k revealed half antitubercular activity (minimal inhibitory concentration = 1.56 μg/ml) than the acetyl analog 6c (minimal inhibitory concentration = 0.78 μg/ml), however, it exhibited more potent broad spectrum antibacterial and antifungal activities in addition to its excellent safety profile with high selectivity toward M. tuberculosis over normal human lung cells. Collectively, these data suggested that compound 6k can be considered as an ideal lead compound for further optimization.

Topics: Antitubercular Agents; Cell Line; Drug Design; Humans; Microbial Sensitivity Tests; Mycobacterium tuberculosis; Structure-Activity Relationship; Thiazoles; Thiazolidines; Tuberculosis