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

Research output: Contribution to journalArticle

48 Citations (Scopus)

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.
LanguageEnglish
Pages624-627
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number3
DOIs
Publication statusPublished - Feb 2007

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Sodium Compounds
Antimony Sodium Gluconate
Poisons
Benzodiazepines
Coinfection
Drug Resistance
HIV Infections
Macrophages
Morbidity
Pharmaceutical Preparations
Toxicity
In Vitro Techniques

Keywords

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

Cite this

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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.",
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Identification of the benzodiazepines as a new class of antileishmanial agent. / Clark, Rachael L.; Carter, Katharine C.; Mullen, Alexander B.; Coxon, Geoffrey D.; Owusu-Dapaah, George; McFarlane, Emma; Dao Duong Thi, M.; Grant, M.H.; Tettey, J.N.A.; Mackay, Simon P.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 3, 02.2007, p. 624-627.

Research output: Contribution to journalArticle

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AU - Carter, Katharine C.

AU - Mullen, Alexander B.

AU - Coxon, Geoffrey D.

AU - Owusu-Dapaah, George

AU - McFarlane, Emma

AU - Dao Duong Thi, M.

AU - Grant, M.H.

AU - Tettey, J.N.A.

AU - Mackay, Simon P.

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KW - bioengineering

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