Design of a novel class of biphenyl CETP inhibitors

被引:15
作者
Lu, Zhijian [1 ]
Napolitano, Joann B. [1 ]
Theberge, Ashleigh [1 ]
Ali, Amjad [1 ]
Hammond, Milton L. [1 ]
Tan, Eugene [1 ]
Tong, Xinchun [1 ]
Xu, Suoyu S. [1 ]
Latham, Melanie J. [2 ]
Peterson, Laurence B. [2 ]
Anderson, Matt S. [3 ]
Eveland, Suzanne S. [3 ]
Guo, Qiu [3 ]
Hyland, Sheryl A. [3 ]
Milot, Denise P. [3 ]
Chen, Ying [3 ]
Sparrow, Carl P. [3 ]
Wright, Samuel D. [3 ]
Sinclair, Peter J. [1 ]
机构
[1] Merck Sharp & Dohme Corp, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Sharp & Dohme Corp, Dept Pharmacol, Rahway, NJ 07065 USA
[3] Merck Sharp & Dohme Corp, Dept Atherosclerosis & Endocrinol, Rahway, NJ 07065 USA
关键词
CETP inhibitors; HDL-C; Biphenyl; ESTER TRANSFER PROTEIN; HIGH-DENSITY-LIPOPROTEIN; TORCETRAPIB; CORONARY; CHOLESTEROL; POTENT; HDL; NIACIN; RISK; 2-ARYLBENZOXAZOLES;
D O I
10.1016/j.bmcl.2010.10.019
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound (12d) has shown an ability to raise HDL significantly in transgenic mouse PD model. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:7469 / 7472
页数:4
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