Targeting ACE and ECE with dual acting inhibitors

Stephen Hanessian; Sébastien Guesné; Ludivine Riber; Julien Marin; Alain Benoist; Philippe Mennecier; Alain Rupin; Tony J Verbeuren; Guillaume De Nanteuil

doi:10.1016/j.bmcl.2007.12.013

Targeting ACE and ECE with dual acting inhibitors

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1058-62. doi: 10.1016/j.bmcl.2007.12.013. Epub 2007 Dec 10.

Authors

Stephen Hanessian¹, Sébastien Guesné, Ludivine Riber, Julien Marin, Alain Benoist, Philippe Mennecier, Alain Rupin, Tony J Verbeuren, Guillaume De Nanteuil

Affiliation

¹ Department of Chemistry, Université de Montréal, PO Box 6128, Station Centre-Ville, Montréal, QB, Canada. stephen.hanessian@umontreal.ca

PMID: 18160283
DOI: 10.1016/j.bmcl.2007.12.013

Abstract

A series of urea analogues related to SA6817 and a GSK phosphonic acid with reported ACE inhibitory activity were prepared and tested for dual ACE and ECE activities. Although excellent ACE and NEP inhibition was achieved, only modest ECE inhibition was observed with one analogue.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Angiotensin-Converting Enzyme Inhibitors / chemical synthesis
Angiotensin-Converting Enzyme Inhibitors / pharmacology*
Aspartic Acid Endopeptidases / antagonists & inhibitors*
Aspartic Acid Endopeptidases / pharmacology*
Combinatorial Chemistry Techniques*
Endothelin-Converting Enzymes
Humans
Metalloendopeptidases / antagonists & inhibitors*
Metalloendopeptidases / pharmacology*
Molecular Structure
Naphthalenes / chemical synthesis
Naphthalenes / chemistry
Naphthalenes / pharmacology*
Stereoisomerism
Structure-Activity Relationship
Urea / analogs & derivatives*
Urea / chemical synthesis
Urea / chemistry
Urea / pharmacology*

Substances

Angiotensin-Converting Enzyme Inhibitors
Naphthalenes
SA6817
Urea
Aspartic Acid Endopeptidases
Metalloendopeptidases
Endothelin-Converting Enzymes