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Pharmacokinetics, metabolism, and in vivo efficacy of the antimalarial natural product bromophycolide A.

ABSTRACT: A suite of pharmacokinetic and pharmacological studies show that bromophycolide A (1), an inhibitor of drug-sensitive and drug-resistant Plasmodium falciparum, displays a typical small molecule profile with low toxicity and good bioavailability. Despite susceptibility to liver metabolism and a short in vivo half-life, 1 significantly decreased parasitemia in a malaria mouse model. Combining these data with prior SAR analyses, we demonstrate the potential for future development of 1 and its bioactive ester analogs.

SUBMITTER: Teasdale ME

PROVIDER: S-EPMC3804352 | biostudies-literature | 2013 Oct

REPOSITORIES: biostudies-literature

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Pharmacokinetics, metabolism, and in vivo efficacy of the antimalarial natural product bromophycolide A.

Teasdale Margaret E ME Prudhomme Jacques J Torres Manuel M Braley Matthew M Cervantes Serena S Bhatia Shanti C SC La Clair James J JJ Le Roch Karine K Kubanek Julia J

ACS medicinal chemistry letters 20131001 10

A suite of pharmacokinetic and pharmacological studies show that bromophycolide A (1), an inhibitor of drug-sensitive and drug-resistant Plasmodium falciparum, displays a typical small molecule profile with low toxicity and good bioavailability. Despite susceptibility to liver metabolism and a short in vivo half-life, 1 significantly decreased parasitemia in a malaria mouse model. Combining these data with prior SAR analyses, we demonstrate the potential for future de ...[more]

PMID: 24159368

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