Identification of the benzodiazepines as a new class of antileishmanial agent

Clark, Rachael L. and Carter, Katharine C. and Mullen, Alexander B. and Coxon, Geoffrey D. and Owusu-Dapaah, George and McFarlane, Emma and Dao Duong Thi, M. and Grant, M.H. and Tettey, J.N.A. and Mackay, Simon P. (2007) Identification of the benzodiazepines as a new class of antileishmanial agent. Bioorganic and Medicinal Chemistry Letters, 17 (3). pp. 624-627. ISSN 0960-894X (http://dx.doi.org/10.1016/j.bmcl.2006.11.004)

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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.