Preparation and in-vitro evaluation of 4-benzylsulfanylpyridine-2-carbohydrazides as potential antituberculosis agents

Arch Pharm (Weinheim). 2009 Jul;342(7):394-404. doi: 10.1002/ardp.200800227.

Abstract

A set of 4-benzylsulfanylpyridine-2-carbohydrazides was synthesized and evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, non-tuberculous mycobacteria, and multidrug-resistant M. tuberculosis. The activities expressed as the minimum inhibitory concentration (MIC) fall into a range of 2 to 125 micromol/L, most often 4 to 32 micromol/L. The results revealed that the substituents on the benzyl moiety do not influence the antimycobacterial efficacy. The substances exhibited similar activities against sensitive and resistant strains of M. tuberculosis. Furthermore, compounds show low antiproliferative effect and cytotoxicity.

MeSH terms

  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Antitubercular Agents / toxicity
  • Cell Death / drug effects
  • Cell Line
  • Cell Proliferation / drug effects
  • Drug Resistance, Multiple, Bacterial
  • Humans
  • Hydrazines / chemical synthesis*
  • Hydrazines / chemistry
  • Hydrazines / pharmacology*
  • Hydrazines / toxicity
  • In Vitro Techniques
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Structure
  • Mycobacterium / drug effects
  • Mycobacterium tuberculosis / drug effects
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Pyridines / pharmacology*
  • Pyridines / toxicity
  • Tuberculosis, Pulmonary / drug therapy
  • Tuberculosis, Pulmonary / microbiology

Substances

  • Antitubercular Agents
  • Hydrazines
  • Pyridines