Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives

Eur J Med Chem. 2010 Oct;45(10):4418-26. doi: 10.1016/j.ejmech.2010.06.036. Epub 2010 Jul 3.

Abstract

As a continuation of our research and with the aim of obtaining new anti-tuberculosis agents which can improve the current chemotherapeutic anti-tuberculosis treatments, forty-three new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives were synthesized and evaluated for in vitro anti-tuberculosis activity against Mycobacterium tuberculosis strain H(37)Rv. Active compounds were also screened to assess toxicity to a VERO cell line. Results indicate that compounds with a methyl moiety substituted in position 3 and unsubstituted benzyl substituted on the carboxamide group provide an efficient approach for further development of anti-tuberculosis agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry
  • Amides / pharmacology
  • Animals
  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / chemistry*
  • Antitubercular Agents / pharmacology*
  • Cell Survival / drug effects
  • Chlorocebus aethiops
  • Humans
  • Mycobacterium tuberculosis / drug effects*
  • Oxides / chemical synthesis
  • Oxides / chemistry
  • Oxides / pharmacology
  • Quinoxalines / chemical synthesis
  • Quinoxalines / chemistry*
  • Quinoxalines / pharmacology*
  • Tuberculosis / drug therapy
  • Vero Cells

Substances

  • Amides
  • Antitubercular Agents
  • Oxides
  • Quinoxalines