Referenced in: none

Automatically associated channels: Kv11.1

Title: 3,4-Diarylpiperidines as potent renin inhibitors.

Authors: Patrick Lacombe, Mélissa Arbour, Renée Aspiotis, Elizabeth Cauchon, Austin Chen, Daniel Dubé, Jean-Pierre Falgueyret, Pierre-André Fournier, Michel Gallant, Erich Grimm, Yongxin Han, Hélène Juteau, Suzanna Liu, Christophe Mellon, Yeeman Ramtohul, Daniel Simard, René St-Jacques, Gavin Chit Tsui

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 Mar 1 , 22, 1953-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22325946

Abstract
The discovery and SAR of a series of potent renin inhibitors possessing a novel 3,4-diarylpiperidine scaffold are described herein. The resulting compound 38 exhibit low nanomolar plasma renin IC(50), had a clean CYP 3A4 profile and displayed micromolar affinity for the hERG channel. Furthermore, it was found to be efficacious in the double transgenic rat hypertension model and show good to moderate oral bioavailability in two animal species.