TY - JOUR
T1 - Identification of the benzodiazepines as a new class of antileishmanial agent
AU - Clark, Rachael L.
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.
PY - 2007/2
Y1 - 2007/2
N2 - 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.
AB - 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.
KW - antileishmanial agents
KW - amastigote
KW - benzodiazepine
KW - pyrrolobenzodiazepine
KW - bioengineering
KW - paullone
UR - http://dx.doi.org/10.1016/j.bmcl.2006.11.004
U2 - 10.1016/j.bmcl.2006.11.004
DO - 10.1016/j.bmcl.2006.11.004
M3 - Article
VL - 17
SP - 624
EP - 627
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 3
ER -
