Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform

被引：83

作者：

Rano, Thomas A. ^{[1
]}

Sieber-McMaster, Ellen ^{[1
]}

Pelton, Patricia D. ^{[1
]}

Yang, Maria ^{[1
]}

Demarest, Keith T. ^{[1
]}

Kuo, Gee-Hong ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Metab Disorders Team, Raritan, NJ 08869 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 09期

关键词：

CETP; Cholesteryl ester transfer protein; HDL-C; Atherosclerosis;

D O I：

10.1016/j.bmcl.2009.03.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tetrahydroquinoline A is a potent inhibitor of the cholesterol ester transfer protein ( CETP), a target for the treatment of low HDL-C and atherosclerosis. Low HDL-C has been identified as a key risk factor for cardiovascular disease in addition to high LDL-C, the target of the statin drugs. Tetrahydroquinoline A inhibits partially purified CETP with an IC50 of 39 nM. The preparation of a series of potent inhibitors of CETP designed around a 1,2,3,4-tetrahydroquinoline platform will be discussed. (c) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2456 / 2460

页数：5

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