卡里希诺醇B的合成及其强效抗疟活性
Synthesis and potent antimalarial activity of kalihinol B.
作者信息
Daub Mary Elisabeth, Prudhomme Jacques, Le Roch Karine, Vanderwal Christopher D
机构信息
†Department of Chemistry, University of California, Irvine, 1102 Natural Sciences II, Irvine, California 92697-2025, United States.
‡Department of Cell Biology and Neuroscience, University of California, Riverside, 900 University Avenue, Riverside, California 92521, United States.
出版信息
J Am Chem Soc. 2015 Apr 22;137(15):4912-5. doi: 10.1021/jacs.5b01152. Epub 2015 Apr 9.
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.
在迄今为止报道的50多种卡里希纳二萜类化合物中，尽管卡里希醇A是较大的抗疟异氰基萜类化合物家族成员中最有效的，但只有5种进行了抗疟活性测试。我们已经验证了一种策略，该策略通过对卡里希醇B（卡里希醇A的四氢呋喃异构体，一种四氢吡喃）进行12步对映选择性合成，来获取许多卡里希纳类化合物。卡里希醇B对氯喹耐药的恶性疟原虫显示出同样高的效力。
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