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

  • Bioorg Med Chem Lett. 2015 Jun 1;25(11):2390-4. doi: 10.1016/j.bmcl.2015.04.009.
Pathi Suman  1 ,  Cherupally Dayakar  1 ,  Kommera Rajkumar  1 ,  Bomma Yashwanth  2 ,  Perumal Yogeeswari  3 ,  Dharmarajan Sriram  3 ,  Janapala Venkateswara Rao  2 ,  Bhimapaka China Raju  4
Affiliations
  • 1. Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
  • 2. Biology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India.
  • 3. Birla Institute of Technology & Science-Pilani, Hyderabad 500 078, India.
  • 4. Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India. Electronic address: [email protected].
PMID: 25908515 DOI: 10.1016/j.bmcl.2015.04.009
Abstract

1H-1,2,3-Triazolylbenzohydrazides (6a-h and 11a-l) were synthesized from 2-chloronicotinaldehydes and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv strain (ATCC-27294). Seven compounds 6b, 6e,f, 11d, 11h, 11j and 11l displayed potent anti-mycobacterial activity (MIC 2.8-6.2 μM). 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.

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