Enhanced Antimalarial Activity of Novel Synthetic Aculeatin Derivatives.

[摘要]：We report the design, synthesis, and in vitro evaluation of novel polyspirocyclic structures, e.g. I, 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 analogs active on the Plasmodium falciparum 3D7 strain. Moreover, these compds. proved to be potent against Toxoplasma gondii. A no. of features that govern these inhibitions were identified.

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