|
|||||
|
|
Design and optimization of new piperidines as renin inhibitors |
|
| Authors: | Olivier Corminboeuf Olivier Bezençon Corinna Grisostomi ?ubo? Remeň Sylvia Richard-Bildstein Daniel Bur Lars Prade Patrick Hess Panja Strickner Walter Fischli Beat Steiner Alexander Treiber |
| Institution: | Drug Discovery Chemistry & Biochemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland |
| Abstract: | The discovery of a new series of piperidine-based renin inhibitors is described herein. SAR optimization upon the P3 renin sub-pocket is described, leading to the discovery of 9 and 41, two bioavailable renin inhibitors orally active at low doses in a transgenic rat model of hypertension. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |