Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors

被引：10

作者：

Escribano, Ana ^{[1
]}

Mateo, Ana I. ^{[1
]}

Martin de la Nava, Eva M. ^{[1
]}

Mayhugh, Daniel R. ^{[2
]}

Cockerham, Sandra L. ^{[2
]}

Beyer, Thomas P. ^{[2
]}

Schmidt, Robert J. ^{[2
]}

Cao, Guoqing ^{[2
]}

Zhang, Youyan ^{[2
]}

Jones, Timothy M. ^{[2
]}

Borel, Anthony G. ^{[2
]}

Sweetana, Stephanie A. ^{[2
]}

Cannady, Ellen A. ^{[2
]}

Mantlo, Nathan B. ^{[2
]}

机构：

[1] Ctr Invest Lilly, Madrid 28108, Spain

[2] Eli Lilly & Co, Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 11期

关键词：

CETP inhibitor; HDL-c; Tetrahydroquinolines; ESTER TRANSFER PROTEIN; DENSITY-LIPOPROTEIN CHOLESTEROL; CORONARY-HEART-DISEASE; ATHEROSCLEROSIS; HDL; TORCETRAPIB; POTENT; TARGET; 2-ARYLBENZOXAZOLES; TOLERABILITY;

D O I：

10.1016/j.bmcl.2012.04.042

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This letter describes the discovery and SAR optimization of tetrazoyl tetrahydroquinoline derivatives as potent CETP inhibitors. Compound 6m exhibited robust HDL-c increase in hCETP/hApoA1 double transgenic model and favorable pharmacokinetic properties. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：3671 / 3675

页数：5

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