Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors

被引:83
|
作者
Eary, C. Todd [1 ]
Jones, Zachary S. [1 ]
Groneberg, Robert D. [1 ]
Burgess, Laurence E. [1 ]
Mareska, David A. [1 ]
Drew, Mark D. [1 ]
Blake, James F. [1 ]
Laird, Ellen R. [1 ]
Balachari, Devan [1 ]
O'Sullivan, Michael [1 ]
Allen, Andrew [1 ]
Marsh, Vivienne [1 ]
机构
[1] Array BioPharma, Boulder, CO 80301 USA
关键词
cholesteryl ester transfer protein; CETP; HDL; tetrahydoquinoxalines; cholesterol;
D O I
10.1016/j.bmcl.2007.01.112
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Cholesteryl ester transfer protein is a plasma glycoprotein that transfers cholesterol ester between lipoprotein particles. Inhibition of this protein, in vitro and in vivo, produces an increase in plasma high density lipoprotein cholesterol (HE)L-Q. This communication will describe the SAR and svnthesis of a series of substituted tetrahydroquinoxaline CETP inhibitors from early P lead to advanced enantiomerically pure anaiogs. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2608 / 2613
页数:6
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