New 1,4-di-N-oxide-quinoxaline-2-ylmethylene isonicotinic acid hydrazide derivatives as anti-Mycobacterium tuberculosis agents

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3699-703. doi: 10.1016/j.bmcl.2011.04.072. Epub 2011 Apr 27.

Abstract

The increase in the prevalence of drug-resistant tuberculosis cases demonstrates the need of discovering new and promising compounds with antimycobacterial activity. As a continuation of our research and with the aim of identifying new antitubercular drugs candidates, a new series of quinoxaline 1,4-di-N-oxide derivatives containing isoniazid was synthesized and evaluated for in vitro anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv strain. Moreover, various drug-like properties of new compounds were predicted. Taking into account the biological results and the promising drug-likeness profile of these compounds, make them valid leads for further experimental research.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Cells, Cultured
  • Chlorocebus aethiops
  • Hydrazines / chemical synthesis*
  • Hydrazines / chemistry
  • Hydrazines / pharmacology*
  • Inhibitory Concentration 50
  • Isonicotinic Acids / chemical synthesis
  • Isonicotinic Acids / chemistry
  • Isonicotinic Acids / pharmacology
  • Molecular Structure
  • Mycobacterium tuberculosis / drug effects*
  • Quinoxalines / chemical synthesis
  • Quinoxalines / chemistry
  • Quinoxalines / pharmacology
  • Vero Cells

Substances

  • Anti-Bacterial Agents
  • Hydrazines
  • Isonicotinic Acids
  • Quinoxalines
  • hydrazine