Anti-Mycobacterium tuberculosis agents derived from quinoxaline-2-carbonitrile and quinoxaline-2-carbonitrile 1,4-di-N-oxide

Arzneimittelforschung. 2002;52(2):113-9. doi: 10.1055/s-0031-1299866.

Abstract

In this paper new quinoxaline derivatives with different substituents in positions 3, 6, 7 and 8 are reported. Their biological activities against Mycobacterium tuberculosis have been assessed and most of the 1,4-di-N-oxide derivatives have been shown to strongly inhibit the bacteria growth in the first in vitro screening. One of these N-oxides (4) is a promising candidate due to its good Selectivity Index (7.95). On the other hand, those compounds without N-oxide moieties showed no or very low activity (growth inhibition: 17% and 39%).

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / pharmacology*
  • Chlorocebus aethiops
  • Indicators and Reagents
  • Macrophages / drug effects
  • Macrophages / microbiology
  • Magnetic Resonance Spectroscopy
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects*
  • Nitriles / chemical synthesis*
  • Nitriles / pharmacology*
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / pharmacology*
  • Spectrophotometry, Infrared
  • Spectrophotometry, Ultraviolet
  • Vero Cells

Substances

  • Antineoplastic Agents
  • Antitubercular Agents
  • Indicators and Reagents
  • Nitriles
  • Quinoxalines
  • quinoxaline-2-carbonitrile
  • quinoxaline-2-carbonitrile 1,4-di-N-oxide