The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors

[Display omitted] Recently, trans-disubstituted oxo-aryl-piperidines have been identified as small molecule nonpeptide renin inhibitors for the modulation of hypertension. Herein, we report on the discovery and preparation of a new class of novel cis-disubstituted amino-aryl-piperidines as a mixture...

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Bibliographic Details
Published inBioorganic & medicinal chemistry Vol. 13; no. 1; pp. 59 - 68
Main Authors Cody, Wayne L., Holsworth, Daniel D., Powell, Noel A., Jalaie, Mehran, Zhang, Erli, Wang, Wei, Samas, Brian, Bryant, John, Ostroski, Robert, Ryan, Michael J., Edmunds, Jeremy J.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 03.01.2005
Elsevier Science
Subjects
Animals
Antihypertensive agents
Antihypertensive Agents - chemistry
Antihypertensive Agents - pharmacology
Biological and medical sciences
Cardiovascular system
Crystallography, X-Ray
Magnetic Resonance Spectroscopy
Medical sciences
Mice
Mice, Transgenic
Pharmacology. Drug treatments
Piperidines - chemistry
Piperidines - pharmacology
Renin - antagonists & inhibitors
Stereoisomerism
Enzyme
Rodentia
Enzyme inhibitor
Non peptide compound
In vitro
Naphthalene derivatives
Biological activity
Cis stereoisomer
Peptidases
In vivo
Vertebrata
Mammalia
Renin
Mouse
Animal
Enantiomer
Modulation
Piperidine derivatives
Hydrolases
Antihypertensive agent
Benzenic compound
Aspartic endopeptidases
Models
Chemical synthesis
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Summary:[Display omitted] Recently, trans-disubstituted oxo-aryl-piperidines have been identified as small molecule nonpeptide renin inhibitors for the modulation of hypertension. Herein, we report on the discovery and preparation of a new class of novel cis-disubstituted amino-aryl-piperidines as a mixture of enantiomers that are potent in vitro renin inhibitors and also, possess in vivo antihypertensive activity in a double transgenic mouse model.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2004.09.056