Identification of the benzodiazepines as a new class of antileishmanial agent.
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.
Clark
Rachel L
RL
Strathclyde Institute for Pharmacy and Biomedical Sciences, University of Strathclyde, 27 Taylor Street, Glasgow G4 0NR, UK.
Carter
Katharine C
KC
Mullen
Alexander B
AB
Coxon
Geoffrey D
GD
Owusu-Dapaah
George
G
McFarlane
Emma
E
Duong Thi
M Dao
MD
Grant
M Helen
MH
Tettey
Justice N A
JN
Mackay
Simon P
SP
D000818:Animals; D000967:Antimony Sodium Gluconate / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007202:Indicators and Reagents; D007891:Leishmania / Q000187:drug effects*; D007893:Leishmania donovani / Q000187:drug effects; D007928:Lethal Dose 50; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology
D000981:Antiprotozoal Agents; D007202:Indicators and Reagents; D001569:Benzodiazepines; D000967:Antimony Sodium Gluconate