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

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ID: 104492
2019
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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 a hydrazide-hydrazone bond were synthesised and evaluated against H37Rv (MTB). The compounds were also evaluated for cytotoxicity against HeLa cell lines. These compounds showed significant activity (MIC) against MTB in the range of 0.2-8 μM without any cytotoxic effects. Compounds (MIC; 0.9 μM), (MIC; 0.2 μM), (MIC; 0.8 μM) and compound (MIC; 0.8 μM), the most active compounds in this series, demonstrate activities on par with INH and superior to those reported for the fluoroquinolones. The SAR analysis suggests that the nature of substituents at positions -1 and -3 of the quinolone nucleus influences anti-MTB activity. Aqueous solubility evaluation and metabolic stability of compound highlights favourable drug-like properties for this compound class.
Reference Key
beteck2019quinoloneisoniazidmedchemcomm Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Beteck, Richard M;Seldon, Ronnett;Jordaan, Audrey;Warner, Digby F;Hoppe, Heinrich C;Laming, Dustin;Legoabe, Lesetja J;Khanye, Setshaba D;
Journal medchemcomm
Year 2019
DOI
10.1039/c8md00480c
URL
Keywords
Cancer mitochondria fluorescence hydrazide-hydrazone h-bonding

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