Aims:
The study aims to synthesize bioactive hybrid pharmacophores (thiazole ring and imidazo[2,1-b]thiazole system) by incorporating them to one biological assessment molecular system.
Background:
Literature survey revealed that various imidazo[2,1-b]thiazoles, thiazoles and hydrazones have powerful anti-mycobacterial activity.
Objective:
This study demonstrates the effectiveness of molecular hybridization and the scope for imidazo[2,1-b]thiazole-hydrazone-thiazoles to develop as promising anti-mycobacterial agents.
Method:
Several imidazo[2,1-b]thiazole–hydrazine-thiazoles 5a-g, 7a,b, 9a,b, 11a,b, 13, and 15a,b were generated using a molecular hybridization strategy and assessed against Mycobacterium tuberculosis (ATCC 25618) for their in vitro antituberculous activity.
Result:
Derivative 7b (MIC = 0.98 μg/mL) has shown the most promising anti-mycobacterial activity among the series tested. Brief structure-activity relationship studies found that the thiazole of chlorophenyl or pyridine or coumarin had a significant relation with the anti-mycobacterial activity.
Conclusion:
Promising anti-mycobacterial activity of compound 7b compared with reference drug suggests that this compound may contribute as a lead compound in search of new potential anti-mycobacterial agents.