title: Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors.
abstract: We have found that both enantiomeric configurations of the 6-alkoxymethyl-1-aryl-2-piperazinone scaffold display equipotent renin inhibition activity and similar SAR patterns. This enantiomeric flexibility is in contrast to a previously reported 3-alkoxymethyl-4-arylpiperidine scaffold.
authors.affiliation: Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. noel.powell@pfizer.com
authors.forename: Noel A
authors.initials: NA
authors.lastname: Powell
authors.forename: Emma H
authors.initials: EH
authors.lastname: Clay
authors.forename: Daniel D
authors.initials: DD
authors.lastname: Holsworth
authors.forename: John W
authors.initials: JW
authors.lastname: Bryant
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Ryan
authors.forename: Mehran
authors.initials: M
authors.lastname: Jalaie
authors.forename: Erli
authors.initials: E
authors.lastname: Zhang
authors.forename: Jeremy J
authors.initials: JJ
authors.lastname: Edmunds
mesh_terms: D001665:Binding Sites; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007202:Indicators and Reagents; D008968:Molecular Conformation; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011487:Protein Conformation; D012083:Renin / Q000737:chemistry; D013237:Stereoisomerism; D000092502:Renin Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D010879:Piperazines; D012083:Renin; D000092502:Renin Inhibitors