Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors.
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.
Powell
Noel A
NA
Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. noel.powell@pfizer.com
Clay
Emma H
EH
Holsworth
Daniel D
DD
Bryant
John W
JW
Ryan
Michael J
MJ
Jalaie
Mehran
M
Zhang
Erli
E
Edmunds
Jeremy J
JJ
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
D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D010879:Piperazines; D012083:Renin; D000092502:Renin Inhibitors