2. Academic Validation
  3. Enhanced antimalarial activity of novel synthetic aculeatin derivatives

Enhanced antimalarial activity of novel synthetic aculeatin derivatives

  • J Med Chem. 2008 Aug 28;51(16):4870-3. doi: 10.1021/jm8007322.
Marine Peuchmaur 1,  Nadia Saïdani,  Cyrille Botté,  Eric Maréchal,  Henri Vial,  Yung-Sing Wong
Affiliations

Affiliation

  • 1 Département de Pharmacochimie Moléculaire, Université de Grenoble, CNRS UMR 5063, CNRS ICMG FR 2607, Bâtiment E, 470 Rue de la Chimie, F-38 041 Grenoble Cedex 9, France.
PMID: 18680278 DOI: 10.1021/jm8007322
Abstract

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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