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 (<b>1</b>), an inhibitor of drug-sensitive and drug-resistant <i>Plasmodium falciparum</i>, displays a typical small molecule profile with low toxicity and good bioavailability. Despite susceptibility to liver metabolism and a short <i>in vivo</i> half-life, <b>1</b> significantly decreased parasitemia in a malaria mouse model. Combining these data with prior SAR analyses, we demonstrate the potential for future development of <b>1</b> and its bioactive ester analogs.