Synthesis and preliminary in vitro evaluation of antimycobacterial activity of new pyrrolo[1,2-a] quinoxaline-carboxylic acid hydrazide derivatives

J Enzyme Inhib Med Chem. 2004 Dec;19(6):489-95. doi: 10.1080/14756360412331280464.

Abstract

New pyrrolo[1,2-a]quinoxaline-2- or -4-carboxylic acid hydrazide derivatives were synthesized from nitroaniline or 1,2-phenylenediamine, and evaluated in vitro for their antimycobacterial activity as part of a TAACF TB screening program. Two compounds 7c and 13 showed an interesting activity at 6.25 microg/mL against Mycobacterium tuberculosis H37Rv, with a 94 and 100 percentage inhibition, respectively.

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacokinetics
  • Carboxylic Acids / chemistry*
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Chlorocebus aethiops
  • Crystallography, X-Ray
  • Drug Evaluation, Preclinical
  • Hydrazines / chemical synthesis*
  • Hydrazines / chemistry
  • Hydrazines / pharmacology*
  • In Vitro Techniques
  • Models, Molecular
  • Molecular Structure
  • Mycobacterium tuberculosis / drug effects*
  • Quinoxalines / chemistry*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Vero Cells

Substances

  • Anti-Bacterial Agents
  • Antitubercular Agents
  • Carboxylic Acids
  • Hydrazines
  • Quinoxalines