(-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor

被引：25

作者：

Kirkup, MP ^{[1
]}

Rizvi, R ^{[1
]}

Shankar, BB ^{[1
]}

Dugar, S ^{[1
]}

Clader, JW ^{[1
]}

McCombie, SW ^{[1
]}

Lin, SI ^{[1
]}

Yumibe, N ^{[1
]}

Huie, K ^{[1
]}

VanHeek, M ^{[1
]}

Compton, DS ^{[1
]}

Davis, HR ^{[1
]}

McPhail, AT ^{[1
]}

机构：

[1] DUKE UNIV,PAUL M GROSS CHEM LAB,DURHAM,NC 27708

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 17期

关键词：

D O I：

10.1016/0960-894X(96)00365-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Previous SAR studies of C-3 side chain modified analogs of (-)-SCH 48461,(1,3,4) as well as information concerning the metabolic stability this series, enabled us to design a cholesterol absorption inhibitor (i.e., (-) 2a, SCH 57939) with tenfold higher potency and greatly enhanced metabolic stability. The synthesis and pharmacological profile, including the role of relative stereochemistry at both the C3 and 1' positions in determining the SAR of these compounds, will be discussed. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2069 / 2072

页数：4

共 9 条

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