Heterocyclic-2-carboxylic acid (3-cyano-1,4-di-N-oxidequinoxalin-2-yl)amide derivatives as hits for the development of neglected disease drugs

Molecules. 2009 Jun 22;14(6):2256-72. doi: 10.3390/molecules14062256.

Abstract

Neglected diseases represent a major health problem. It is estimated that one third of the world population is infected with tuberculosis (TB). Besides TB, Chagas disease, affects approximately 20 million people. Quinoxalines display great activities against TB and Chagas. Forty new quinoxaline 1,4-di-N-oxide derivatives have been prepared and tested against M. tuberculosis and T. cruzi. Carboxylic acid quinoxaline 1,4-di-N-oxides (CAQDOs) 5 and 17 showed MIC values on the same order as the reference antituberculosis drug, rifampicin. Meanwhile, CAQDOs 12 and 22 presented IC(50) values in the same order as the anti-chagasic drug, nifurtimox.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antitubercular Agents / chemistry*
  • Antitubercular Agents / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Mycobacterium tuberculosis / drug effects
  • Quinoxalines / chemistry*
  • Quinoxalines / pharmacology*
  • Rifampin
  • Trypanosoma / drug effects

Substances

  • Antitubercular Agents
  • Quinoxalines
  • Rifampin