Identification of the benzodiazepines as a new class of antileishmanial agent

Bioorg Med Chem Lett. 2007 Feb 1;17(3):624-7. doi: 10.1016/j.bmcl.2006.11.004. Epub 2006 Nov 6.

Abstract

The continual increase in drug resistance; the lack of new chemotherapeutic agents; the toxicity of existing agents and the increasing morbidity with HIV co-infection mean the search for new antileishmanial agents has never been more urgent. We have identified the benzodiazepines as a structural class for antileishmanial hit optimisation, and demonstrated that their in vitro activity is comparable with the clinically used drug, sodium stibogluconate, and that the compounds are not toxic to macrophages.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimony Sodium Gluconate / pharmacology
  • Antiprotozoal Agents / chemical synthesis*
  • Antiprotozoal Agents / pharmacology*
  • Antiprotozoal Agents / toxicity
  • Benzodiazepines / chemical synthesis*
  • Benzodiazepines / pharmacology*
  • Benzodiazepines / toxicity
  • Indicators and Reagents
  • Leishmania / drug effects*
  • Leishmania donovani / drug effects
  • Lethal Dose 50
  • Macrophages / drug effects
  • Macrophages / parasitology

Substances

  • Antiprotozoal Agents
  • Indicators and Reagents
  • Benzodiazepines
  • Antimony Sodium Gluconate