Synthesis of New Thiazole Clubbed Imidazo[2,1-b]thiazole Hybrid as Antimycobacterial Agents

Aims: The study aims to synthesize bioactive hybrid pharmacophores (thiazole ring and imidazo[2,1-b]thiazole system) by incorporating them into one biological assessment molecular system. Background: A literature survey revealed that various imidazo[2,1-b]thiazoles, thiazoles, and hydrazones have powerful antimycobacterial 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 antimycobacterial agents. Methods: 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. Results: Derivative 7b (MIC = 0.98 mu g/mL) has shown the most promising antimycobacterial 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 antimycobacterial activity. Conclusion: The promising antimycobacterial activity of compound 7b compared with the reference drug suggests that this compound may contribute as a lead compound in the search for new potential antimycobacterial agents.

Automated summary

This study aims to synthesize bioactive hybrid pharmacophores and assess their antimycobacterial activity. The results showed that derivative 7b exhibited the most promising antimycobacterial activity among the tested compounds. The structure-activity relationship studies indicated that the substituent on the thiazole ring was related to the antimycobacterial activity.