Ontology highlight
ABSTRACT:
SUBMITTER: Gujjar R
PROVIDER: S-EPMC2746568 | biostudies-literature | 2009 Apr
REPOSITORIES: biostudies-literature
Gujjar Ramesh R Marwaha Alka A El Mazouni Farah F White John J White Karen L KL Creason Sharon S Shackleford David M DM Baldwin Jeffrey J Charman William N WN Buckner Frederick S FS Charman Susan S Rathod Pradipsinh K PK Phillips Margaret A MA
Journal of medicinal chemistry 20090401 7
Plasmodium falciparum causes 1-2 million deaths annually. Yet current drug therapies are compromised by resistance. We previously described potent and selective triazolopyrimidine-based inhibitors of P. falciparum dihydroorotate dehydrogenase (PfDHODH) that inhibited parasite growth in vitro; however, they showed no activity in vivo. Here we show that lack of efficacy against P. berghei in mice resulted from a combination of poor plasma exposure and reduced potency against P. berghei DHODH. For ...[more]