Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors

Noel A Powell; Emma H Clay; Daniel D Holsworth; John W Bryant; Michael J Ryan; Mehran Jalaie; Erli Zhang; Jeremy J Edmunds

doi:10.1016/j.bmcl.2005.02.085

Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors

Bioorg Med Chem Lett. 2005 May 2;15(9):2371-4. doi: 10.1016/j.bmcl.2005.02.085.

Authors

Noel A Powell¹, Emma H Clay, Daniel D Holsworth, John W Bryant, Michael J Ryan, Mehran Jalaie, Erli Zhang, Jeremy J Edmunds

Affiliation

¹ Pfizer Global Research and Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. noel.powell@pfizer.com

PMID: 15837327
DOI: 10.1016/j.bmcl.2005.02.085

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.

MeSH terms

Binding Sites
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Indicators and Reagents
Molecular Conformation
Molecular Structure
Piperazines / chemical synthesis*
Piperazines / chemistry
Piperazines / pharmacology*
Protein Conformation
Renin / antagonists & inhibitors*
Renin / chemistry
Stereoisomerism

Substances

Enzyme Inhibitors
Indicators and Reagents
Piperazines
Renin