Synthesis and antitubercular activity of a series of hydrazone and nitrovinyl analogs derived from heterocyclic aldehydes

J Enzyme Inhib Med Chem. 2009 Feb;24(1):117-24. doi: 10.1080/14756360801915526.

Abstract

A series of hydrazone and 3-nitrovinyl analogs of indole-3-carboxaldehydes and related compounds were synthesized and screened for antitubercular activity against Mycobacterium tuberculosis H37R(V) in BACTEC 12B medium using the Microplate Alamar Blue Assay (MABA). Several compounds showed inhibitory activity against M. tuberculosis in primary screening assays at a concentration of 6.25 microg/mL; subsequent dose-response studies indicated that the most active compounds, 3d, 3e & 8b, had IC(50) values of 5.96, 5.4 & 1.6 microg/mL, respectively. These compounds represent potential leads for the further development of novel antitubercular agents.

MeSH terms

  • Aldehydes / chemistry
  • Antitubercular Agents / chemical synthesis*
  • Dose-Response Relationship, Drug
  • Hydrazones / chemical synthesis*
  • Hydrazones / pharmacology
  • Inhibitory Concentration 50
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects
  • Vinyl Compounds / chemical synthesis*
  • Vinyl Compounds / pharmacology

Substances

  • Aldehydes
  • Antitubercular Agents
  • Hydrazones
  • Vinyl Compounds