Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors

被引:32
作者
Pfefferkorn, Jeffrey A. [1 ]
Choi, Chulho [1 ]
Song, Yuntao [1 ]
Trivedi, Bharat K. [1 ]
Larsen, Scott D. [1 ]
Askew, Valerie [1 ]
Dillon, Lisa [1 ]
Hanselman, Jeffrey C. [1 ]
Lin, Zhiwu [1 ]
Lu, Gina [1 ]
Robertson, Andrew [1 ]
Sekerke, Catherine [1 ]
Auerbach, Bruce [1 ]
Pavlovsky, Alexander [1 ]
Harris, Melissa S. [1 ]
Bainbridge, Graeme [1 ]
Caspers, Nicole [1 ]
机构
[1] Pfizer Global Res & Dev, Michigan Labs, Ann Arbor, MI 48105 USA
关键词
HMG-CoA reductase inhibitor; statin; Hypercholesterolemia;
D O I
10.1016/j.bmcl.2007.05.097
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase were discovered. Leading analogs demonstrated potent inhibition of cholesterol synthesis in both in vitro and in vivo models and may be useful for the treatment of hypercholesterolemia and related lipid disorders. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4531 / 4537
页数:7
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