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角鲨菌素,一种茎点霉属菌株产生的新型鲨烯合酶抑制剂。II. 结构解析。

The squalestatins, novel inhibitors of squalene synthase produced by a species of Phoma. II. Structure elucidation.

作者信息

Sidebottom P J, Highcock R M, Lane S J, Procopiou P A, Watson N S

机构信息

Structural Chemistry Department, Glaxo Group Research Limited, Greenford, Middlesex, United Kingdom.

出版信息

J Antibiot (Tokyo). 1992 May;45(5):648-58. doi: 10.7164/antibiotics.45.648.

Abstract

Three novel fungal metabolites 1-3 isolated from cultures of a Phoma sp. C2932, are potent and selective inhibitors of squalene synthase. Their structures have been determined by a combination of spectroscopic, X-ray crystallographic and chemical methods; these natural products incorporate the highly functionalised bicyclic core, [1S-(1 alpha, 3 alpha, 4 beta, 5 alpha, 6 alpha, 7 beta]-4,6,7-trihydroxy- 2,8-dioxabicyclo-[3.2.1]octane-3,4,5-tricarboxylic acid.

摘要

从茎点霉属真菌Phoma sp. C2932的培养物中分离出的三种新型真菌代谢产物1-3是角鲨烯合酶的强效和选择性抑制剂。它们的结构已通过光谱、X射线晶体学和化学方法相结合确定;这些天然产物包含高度官能化的双环核心,即[1S-(1α, 3α, 4β, 5α, 6α, 7β)]-4,6,7-三羟基-2,8-二氧杂双环-[3.2.1]辛烷-3,4,5-三羧酸。

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