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Enhanced antimalarial activity of novel synthetic aculeatin derivatives.
Journal article   Peer reviewed

Enhanced antimalarial activity of novel synthetic aculeatin derivatives.

Marine Peuchmaur, Nadia Saïdani, Cyrille Botté, Eric Maréchal, Henri Vial and Yung-Sing Wong
Journal of Medicinal Chemistry, Vol.51(16), pp.4870-3
28/08/2008
PMID: 18680278

Abstract

human parasite malaria Plasmodium falciparum drug discovery antimalarial natural product aculeatin synthesis biological activity Alkanes Animals Antimalarials Cyclohexanones Spiro Compounds Structure-Activity Relationship
We report the design, synthesis, and in vitro evaluation of novel polyspirocyclic structures, inspired by the antimalarial natural products, the aculeatins. A divergent synthetic strategy was conceived for the practical supply and has allowed the discovery of two novel and more potent analogues active on the Plasmodium falciparum 3D7 strain. Moreover, these compounds proved to be potent against Toxoplasma gondii. A number of features that govern these inhibitions were identified.
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