Open source drug discovery: highly potent antimalarial compounds derived from the Tres Cantos arylpyrroles (Publications)
The development of new antimalarial compounds remains a pivotal part of the strategy for malaria elimination. Recent large-scale phenotypic screens have provided a wealth of potential starting points for
Discovery of a quinoline-4-carboxamide derivative with a novel mechanism of action, multistage antimalarial activity, and potent in vivo efficacy (Publications)
pharmacokinetic profile led to several compounds showing excellent oral efficacy in the P. berghei malaria mouse model with ED90 values below 1 mg/kg when dosed orally for 4 days. The favorable potency,
Costs and cost-effectiveness of <em>Plasmodium vivax </em>control (Publications)
The continued success of efforts to reduce the global malaria burden will require sustained funding for interventions specifically targeting Plasmodium vivax The optimal use of limited financial resources
Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary... (Publications)
Despite recent progress in the fight against malaria, the emergence and spread of drug-resistant parasites remains a serious obstacle to the treatment of infections. We recently reported the development
Design, synthesis, and evaluation of 5'-diphenyl nucleoside analogues as inhibitors of the <em>Plasmodium falciparum</em> dUTPase (Publications)
Deoxyuridine 5'-triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for malaria. We previously reported some 5'-tritylated deoxyuridine analogues (both cyclic and acyclic) as selective
Structure-activity relationship studies of pyrrolone antimalarial agents (Publications)
mammalian (L6) cells. Three representative compounds were selected for evaluation in a rodent model of malaria infection, and the best compound showed improved ability to decrease parasitaemia and a slight increase
Evaluation of ethnobotanically selected Benin medicinal plants for their in vitro antiplasmodial activity (Publications)
Twenty extracts from nine Benin medicinal plants, traditionally used to treat malaria, were screened for in vitro antiplasmodial activity towards Plasmodium falciparum K1 chloroquine resistant and 3D7
Validation of the protein kinase <em>Pf</em>CLK3 as a multistage cross-species malarial drug target (Publications)
target for drugs, with the potential to offer a cure-to be prophylactic and transmission blocking in malaria.
<em>Plasmodium falciparum</em> sexual commitment rate variation among clinical isolates and diverse laboratory-adapted lines (Publications)
Asexual blood-stage malaria parasites must produce sexual progeny to infect mosquitoes. It is important to understand the scope and causes of intraspecific variation in sexual commitment rates, particularly [...] variation of this key reproductive trait that likely affects transmission. IMPORTANCE Only sexual-stage malaria parasites are transmitted from human blood to mosquitoes. Thus, it is vital to understand variations
Comparison of cone bioassay estimates at two laboratories with different <em>Anopheles </em>mosquitoes for quality assurance of pyrethroid... (Publications)
insecticide-treated nets (ITNs) delivered to malaria-endemic countries is conducted by measuring physiochemical parameters, but not bioefficacy against malaria mosquitoes. This study explored utility of