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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2011-07, Vol.21 (13), p.3976-3981
Main Authors: Chen, Austin, Cauchon, Elizabeth, Chefson, Amandine, Dolman, Sarah, Ducharme, Yves, Dubé, Daniel, Falgueyret, Jean-Pierre, Fournier, Pierre-André, Gagné, Sébastien, Gallant, Michel, Grimm, Erich, Han, Yongxin, Houle, Robert, Huang, Jing-Qi, Hughes, Gregory, Jûteau, Hélène, Lacombe, Patrick, Lauzon, Sophie, Lévesque, Jean-François, Liu, Susana, MacDonald, Dwight, Mackay, Bruce, McKay, Dan, Percival, M. David, St-Jacques, René, Toulmond, Sylvie
Format: Article
Language:English
Subjects:
Alcohols - chemical synthesis
Alcohols - chemistry
Alcohols - therapeutic use
Animals
Antihypertensive agents
Antihypertensive Agents - chemical synthesis
Antihypertensive Agents - chemistry
Antihypertensive Agents - therapeutic use
Biological and medical sciences
Cardiovascular system
chemistry
Drug Design
hypertension
Hypertension - drug therapy
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
piperidines
Piperidines - chemical synthesis
Piperidines - chemistry
Piperidines - therapeutic use
Rats
renin
Renin - antagonists & inhibitors
Renin - chemistry
Structure-Activity Relationship
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Description
Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2011.05.014