Identification of the benzodiazepines as a new class of antileishmanial agent

Rachael L. Clark, Katharine C. Carter, Alexander B. Mullen, Geoffrey D. Coxon, George Owusu-Dapaah, Emma McFarlane, M. Dao Duong Thi, M.H. Grant, J.N.A. Tettey, Simon P. Mackay

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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.
Original languageEnglish
Pages (from-to)624-627
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number3
DOIs
Publication statusPublished - Feb 2007

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Keywords

  • antileishmanial agents
  • amastigote
  • benzodiazepine
  • pyrrolobenzodiazepine
  • bioengineering
  • paullone

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