Title:Synthesis of New Thiazole Clubbed Imidazo[2,1-b]thiazole Hybrid as
Antimycobacterial Agents
Volume: 18
Issue: 10
Author(s): Huda K. Mahmoud, Abdelwahed R. Sayed, Marwa M. Abdel-Aziz and Sobhi M. Gomha*
Affiliation:
- Department of Chemistry, Faculty of Science, University of Cairo, Giza, Egypt
- Department of Chemistry, Faculty of Science, Islamic University of Madinah, Madinah 42351, Saudi Arabia
Keywords:
Thiosemicarbazones, imidazothiazole, thiazole, hydrazones, bis-heterocycles, tuberculosis.
Abstract:
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 μg/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.