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2000
Volume 18, Issue 10
  • ISSN: 1573-4064
  • E-ISSN: 1875-6638

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.

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/content/journals/mc/10.2174/1573406418666220413095854
2022-12-01
2025-01-10
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/content/journals/mc/10.2174/1573406418666220413095854
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  • Article Type:
    Research Article
Keyword(s): bis-heterocycles; hydrazones; imidazothiazole; thiazole; Thiosemicarbazones; tuberculosis
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