RESUMEN

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.

Asunto(s)

Antiprotozoarios/síntesis química , Antiprotozoarios/farmacología , Benzodiazepinas/síntesis química , Benzodiazepinas/farmacología , Leishmania/efectos de los fármacos , Animales , Gluconato de Sodio Antimonio/farmacología , Antiprotozoarios/toxicidad , Benzodiazepinas/toxicidad , Indicadores y Reactivos , Leishmania donovani/efectos de los fármacos , Dosificación Letal Mediana , Macrófagos/efectos de los fármacos , Macrófagos/parasitología