STRUCTURALLY SIMPLIFIED SQUALESTATINS - MONOCYCLIC 1,3-DIOXANE ANALOGS

被引:15
|
作者
SHARRATT, PJ
HUTSON, JL
INGLIS, GGA
LESTER, MG
PROCOPIOU, PA
WATSON, NS
机构
[1] Glaxo Group Research Ltd., Greenford
关键词
D O I
10.1016/S0960-894X(01)80175-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Monocyclic analogues of squalestatin 1 based on a 1,3-dioxane ring were prepared and evaluated for their ability to inhibit squalene synthase in vitro. The compound 16a possessing a 4,6-dimethyloctenoyloxymethyl group at C4 and a carboxamide at C2 showed similar inhibitory activity to 1.
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页码:661 / 666
页数:6
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