Renin inhibitors for the treatment of hypertension: Design and optimization of a novel series of tertiary alcohol-bearing piperidines

The design and optimization of a novel series of renin inhibitor is described herein. Strategically, by committing the necessary resources to the development of synthetic sequences and scaffolds that were most amenable for late stage structural diversification, even as the focus of the SAR campaign moved from one end of the molecule to another, highly potent renin inhibitors could be rapidly identified and profiled.

Graphical abstractThe discovery of a novel series of potent, orally-bioavailable renin inhibitor through a rational, structure-guided truncation and optimization campaign.Figure optionsDownload full-size imageDownload as PowerPoint slide