Synthesis and Potent Antimalarial Activity of Kalihinol B

[Image: see text] Of the 50+ kalihinane diterpenoids reported to date, only five had been tested for antimalarial activity, in spite of the fact that kalihinol A is the most potent among the members of the larger family of antimalarial isocyanoterpenes. We have validated a strategy designed to acces...

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Detalles Bibliográficos
Autores principales: Daub, Mary Elisabeth, Prudhomme, Jacques, Le Roch, Karine, Vanderwal, Christopher D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2015
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4415034/
https://www.ncbi.nlm.nih.gov/pubmed/25815413
http://dx.doi.org/10.1021/jacs.5b01152
Descripción
Sumario:[Image: see text] Of the 50+ kalihinane diterpenoids reported to date, only five had been tested for antimalarial activity, in spite of the fact that kalihinol A is the most potent among the members of the larger family of antimalarial isocyanoterpenes. We have validated a strategy designed to access many of the kalihinanes with a 12-step enantioselective synthesis of kalihinol B, the tetrahydrofuran isomer of kalihinol A (a tetrahydropyran). Kalihinol B shows similarly high potency against chloroquine-resistant Plasmodium falciparum.

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