Synthesis and Potent Antimalarial Activity of Kalihinol B

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 kali...

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Vydané v:	Journal of the American Chemical Society Ročník 137; číslo 15; s. 4912 - 4915
Hlavní autori:	Daub, Mary Elisabeth, Prudhomme, Jacques, Le Roch, Karine, Vanderwal, Christopher D
Médium:	Journal Article
Jazyk:	English
Vydavateľské údaje:	WASHINGTON American Chemical Society 22.04.2015 Amer Chemical Soc
Predmet:	Antimalarials - chemical synthesis Antimalarials - chemistry Antimalarials - pharmacology Chemistry Chemistry, Multidisciplinary Chloroquine - pharmacology Diterpenes - chemical synthesis Diterpenes - chemistry Diterpenes - pharmacology Drug Resistance - drug effects Molecular Structure Parasitic Sensitivity Tests Physical Sciences Plasmodium falciparum - drug effects Science & Technology SPONGE ETHER NATURAL-PRODUCTS DITERPENE ISONITRILES RESISTANCE ALDEHYDES TERPENOIDS MICHAEL ADDITION
ISSN:	0002-7863, 1520-5126, 1520-5126
On-line prístup:	Získať plný text
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Shrnutí:	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.
Bibliografia:	NIH RePORTER ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0002-7863 1520-5126 1520-5126
DOI:	10.1021/jacs.5b01152