Targeting ACE and ECE with dual acting inhibitors.
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.
Hanessian
Stephen
S
Department of Chemistry, Université de Montréal, PO Box 6128, Station Centre-Ville, Montréal, QB, Canada. stephen.hanessian@umontreal.ca
Guesné
Sébastien
S
Riber
Ludivine
L
Marin
Julien
J
Benoist
Alain
A
Mennecier
Philippe
P
Rupin
Alain
A
Verbeuren
Tony J
TJ
De Nanteuil
Guillaume
G
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors* / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D000072396:Endothelin-Converting Enzymes; D006801:Humans; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors* / Q000494:pharmacology*; D015394:Molecular Structure; D009281:Naphthalenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000806:Angiotensin-Converting Enzyme Inhibitors; D009281:Naphthalenes; C527344:SA6817; D014508:Urea; D016282:Aspartic Acid Endopeptidases; D008666:Metalloendopeptidases; D000072396:Endothelin-Converting Enzymes