Synthesis and antitubercular activities of acetamide-substituted benzazole derivatives

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Erzincan Üniversitesi Fen Bilimleri Enstitüsü Dergisi
Volume:17 Issue:2
Synthesis and antitubercular activities of acetamide-substituted benzazole derivatives

Synthesis and antitubercular activities of acetamide-substituted benzazole derivatives

Authors : Şule Gürsoy, Elif Şevval Öztürk, Bayan Zoatier, Mahmut Ülger, Öztekin Algül

Pages : 474-487

Doi:10.18185/erzifbed.1480781

View : 53 | Download : 59

Publication Date : 2024-08-31

Article Type : Research Paper

Abstract :Multidrug-resistant Mycobacterium tuberculosis strains\' increasing emergence and rapid spread necessitate the urgent development of innovative antimycobacterial agents. In pursuit of novel agents, a series of N-(benzazole-2-ylmethyl)-2-substituted phenylacetamide or N-(benzazole-2-ylmethyl)-2-(thiophen-2-yl)acetamide compounds (6-11) were synthesized. Their efficacy against multidrug-resistant Mycobacterium tuberculosis was assessed. Compounds exhibited potent antimycobacterial activity with minimum inhibitory concentrations (MIC) ranging from 1.05 to 4.10 µM and demonstrated low cytotoxicity towards fibroblast cell line (L929). ADMET predictions suggested that these synthesized compounds possess drug-like properties. Our findings offer a promising starting point for designing more selective and potent antimycobacterial agents.
Keywords : Benzazole, synthesis, Mycobacterium tuberculosis, MIC, antitubercular activity

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