Synthesis and antituberculosis activity of some N-pyridyl-N'-thiazolylhydrazine derivatives

Eur J Med Chem. 2010 May;45(5):2085-8. doi: 10.1016/j.ejmech.2010.01.017. Epub 2010 Jan 20.

Abstract

In this study, new N-(1-arylethylidene)-N'-(4-arylthiazol-2-yl)hydrazine derivatives were synthesized and evaluated for their antituberculosis activity. The chemical structures of the compounds were elucidated by IR, NMR and FAB+-MS spectral data and Elemental Analyses. The initial screen was conducted against Mycobacterium tuberculosis H37Rv (ATCC 27294) in BACTEC 12B medium using the Microplate Alamar Blue Assay (MABA). The VERO cell cytotoxicity assay was done in parallel with the TB Dose Response assay. Viability was assessed using Promega's Cell Titer-Glo Luminescent Cell Viability Assay. Cytotoxicity was determined from the dose-response curve as the CC50 using a curve-fitting program. One of the compounds showed high activity with low toxicity.

MeSH terms

  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Hydrazines / chemical synthesis*
  • Hydrazines / chemistry
  • Hydrazines / pharmacology*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Mycobacterium tuberculosis / drug effects*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Antitubercular Agents
  • Hydrazines