Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis

Bioorg Med Chem Lett. 2010 Jan 1;20(1):149-52. doi: 10.1016/j.bmcl.2009.11.022. Epub 2009 Nov 14.

Abstract

A series of halo-nitrobenzamide were synthesized and evaluated for their ability to block proliferation of Trypanosoma brucei brucei. A number of these compounds had significant activity against the parasite, particularly 2-chloro-N-(4-chlorophenyl)-5-nitrobenzamide 17 which exhibited low micromolar inhibitory potency against T. brucei and selectivity towards both malaria and mammalian cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzamides / chemical synthesis
  • Benzamides / chemistry*
  • Benzamides / pharmacology
  • Drug Discovery
  • Humans
  • Parasitic Sensitivity Tests
  • Trypanocidal Agents / chemical synthesis
  • Trypanocidal Agents / chemistry*
  • Trypanocidal Agents / pharmacology
  • Trypanosoma brucei brucei / drug effects
  • Trypanosomiasis, African / drug therapy

Substances

  • 2-chloro-N-(4-chlorophenyl)-5-nitrobenzamide
  • Benzamides
  • Trypanocidal Agents