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

Abstract

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.

• Authors: Austin Chen, Elizabeth Cauchon, Amandine Chefson, Sarah Dolman, Yves Ducharme, Daniel Dubé, Jean-Pierre Falgueyret, Pierre-André Fournier, Sébastien Gagné, Michel Gallant, Erich Grimm, Yongxin Han, Robert Houle, Jing-Qi Huang, Gregory Hughes, Hélène Jûteau, Patrick Lacombe, Sophie Lauzon, Jean-François Lévesque, Susana Liu, Dwight Macdonald, Bruce Mackay, Dan McKay, M David Percival, René St-Jacques, Sylvie Toulmond
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 21 Issue 13 Pg. 3976-81 (Jul 01 2011) ISSN: 1464-3405 [Electronic] England
• PMID: 21641209 (Publication Type: Journal Article)
• Copyright: Copyright © 2011 Elsevier Ltd. All rights reserved.

Chemical References

• Alcohols
• Antihypertensive Agents
• Piperidines
• Renin

Topics

• Alcohols (chemical synthesis, chemistry, therapeutic use)
• Animals
• Antihypertensive Agents (chemical synthesis, chemistry, therapeutic use)
• Drug Design
• Hypertension (drug therapy)
• Molecular Structure
• Piperidines (chemical synthesis, chemistry, therapeutic use)
• Rats
• Renin (antagonists & inhibitors, chemistry)
• Structure-Activity Relationship