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

Authors :
Chen A
Cauchon E
Chefson A
Dolman S
Ducharme Y
Dubé D
Falgueyret JP
Fournier PA
Gagné S
Gallant M
Grimm E
Han Y
Houle R
Huang JQ
Hughes G
Jûteau H
Lacombe P
Lauzon S
Lévesque JF
Liu S
Macdonald D
Mackay B
McKay D
Percival MD
St-Jacques R
Toulmond S
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jul 01; Vol. 21 (13), pp. 3976-81. Date of Electronic Publication: 2011 May 14.
Publication Year :
2011

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.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
21
Issue :
13
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
21641209
Full Text :
https://doi.org/10.1016/j.bmcl.2011.05.014