Abstract |
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.
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Authors | Wayne L Cody, Daniel D Holsworth, Noel A Powell, Mehran Jalaie, Erli Zhang, Wei Wang, Brian Samas, John Bryant, Robert Ostroski, Michael J Ryan, Jeremy J Edmunds |
Journal | Bioorganic & medicinal chemistry
(Bioorg Med Chem)
Vol. 13
Issue 1
Pg. 59-68
(Jan 03 2005)
ISSN: 0968-0896 [Print] England |
PMID | 15582452
(Publication Type: Journal Article)
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Chemical References |
- Antihypertensive Agents
- Piperidines
- Renin
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Topics |
- Animals
- Antihypertensive Agents
(chemistry, pharmacology)
- Crystallography, X-Ray
- Magnetic Resonance Spectroscopy
- Mice
- Mice, Transgenic
- Piperidines
(chemistry, pharmacology)
- Renin
(antagonists & inhibitors)
- Stereoisomerism
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