title: 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.
authors.affiliation: Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. wayne.cody@pfizer.com
authors.forename: Wayne L
authors.initials: WL
authors.lastname: Cody
authors.forename: Daniel D
authors.initials: DD
authors.lastname: Holsworth
authors.forename: Noel A
authors.initials: NA
authors.lastname: Powell
authors.forename: Mehran
authors.initials: M
authors.lastname: Jalaie
authors.forename: Erli
authors.initials: E
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Wang
authors.forename: Brian
authors.initials: B
authors.lastname: Samas
authors.forename: John
authors.initials: J
authors.lastname: Bryant
authors.forename: Robert
authors.initials: R
authors.lastname: Ostroski
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Ryan
authors.forename: Jeremy J
authors.initials: JJ
authors.lastname: Edmunds
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000737:chemistry / Q000494:pharmacology; D018360:Crystallography, X-Ray; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008822:Mice, Transgenic; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology*; D013237:Stereoisomerism; D000092502:Renin Inhibitors
chemical_list: D000959:Antihypertensive Agents; D010880:Piperidines; D000092502:Renin Inhibitors