Quinolone-isoniazid hybrids: synthesis and preliminary in vitro cytotoxicity and anti-tuberculosis evaluation.

ABSTRACT: Herein, we propose novel quinolones incorporating an INH moiety as potential drug templates against TB. The quinolone-based compounds bearing an INH moiety attached via a hydrazide-hydrazone bond were synthesised and evaluated against Mycobacterium tuberculosis H37Rv (MTB). The compounds were also evaluated for cytotoxicity against HeLa cell lines. These compounds showed significant activity (MIC₉₀) against MTB in the range of 0.2-8 μM without any cytotoxic effects. Compounds 10 (MIC₉₀; 0.9 μM), 11 (MIC₉₀; 0.2 μM), 12 (MIC₉₀; 0.8 μM) and compound 15 (MIC₉₀; 0.8 μM), the most active compounds in this series, demonstrate activities on par with INH and superior to those reported for the fluoroquin

SUBMITTER: Beteck RM 

PROVIDER: S-EPMC6390685 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature