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

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.
AuthorsWayne 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
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 13 Issue 1 Pg. 59-68 (Jan 03 2005) ISSN: 0968-0896 [Print] England
PMID15582452 (Publication Type: Journal Article)
Chemical References
  • Antihypertensive Agents
  • Piperidines
  • Renin
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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