4.5 Article

Synthesis and anti-mycobacterial activity of 2-chloronicotinaldehydes based novel 1H-1,2,3-triazolylbenzohydrazides

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 11, Pages 2390-2394

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.04.009

Keywords

2-Chloronicotinaldehydes; 1H-1,2,3-Triazolylbenzohydrazides; Click chemistry; Anti-mycobacterial activity; Cytotoxicity

Funding

  1. CSIR, New-Delhi [CSC0108]
  2. CSIR, New Delhi

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1H-1,2,3-Triazolylbenzohydrazides (6a-h and 11a-l) were synthesized from 2-chloronicotinaldehydes and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis H(37)Rv strain (ATCC-27294). Seven compounds 6b, 6e, f, 11d, 11h, 11j and 11l displayed potent anti-mycobacterial activity (MIC 2.8-6.2 mu M). Potent anti-mycobacterial compounds were chosen for cytotoxicity studies by MTT protein assay against normal cell lines (PBMC and Raw 264.7) and shown low cytotoxicity. This is the first Letter assigning anti-mycobacterial activity, cytotoxicity and structure activity relationship for 1H-1,2, 3-triazolylbenzohydrazides. (C) 2015 Elsevier Ltd. All rights reserved.

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