Development of New Antimycobacterial Sulfonyl Hydrazones and 4-Methyl-1,2,3-thiadiazole-Based Hydrazone Derivatives.

ABSTRACT: Fifteen 4-methyl-1,2,3-thiadiazole-based hydrazone derivatives 3a-d and sulfonyl hydrazones 5a-k were synthesized. They were characterized by ¹H-NMR, ¹³C NMR, and HRMS. Mycobacterium tuberculosis strain H37Rv was used to assess their antimycobacterial activity. All compounds demonstrated significant minimum inhibitory concentrations (MIC) from 0.07 to 0.32 µM, comparable to those of isoniazid. The cytotoxicity was evaluated using the standard MTT-dye reduction test against human embryonic kidney cells HEK-293T and mouse fibroblast cell line CCL-1. 4-Hydroxy-3-methoxyphenyl substituted 1,2,3-thiadiazole-based hydrazone derivative 3d demonstrated the highest antimycobacterial activity (MIC = 0.0730 µM) and minimal associated cyt

SUBMITTER: Angelova VT 

PROVIDER: S-EPMC9137698 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature