Substituted piperidines -: Highly potent renin inhibitors due to induced fit adaptation of the active site

被引:98
作者
Vieira, E [1 ]
Binggeli, A [1 ]
Breu, V [1 ]
Bur, D [1 ]
Fischli, W [1 ]
Güller, R [1 ]
Hirth, G [1 ]
Märki, HP [1 ]
Müller, M [1 ]
Oefner, C [1 ]
Scalone, M [1 ]
Stadler, H [1 ]
Wilhelm, M [1 ]
Wostl, W [1 ]
机构
[1] F Hoffmann La Roche & Co Ltd, Pharma Res Dept, CH-4070 Basel, Switzerland
关键词
D O I
10.1016/S0960-894X(99)00195-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The identification, synthesis and activity of a novel class of piperidine renin inhibitors is presented. The most active compounds show activities in the picomolar range and are among the most potent renin inhibitors ever identified. (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1397 / 1402
页数:6
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