Synthesis of N-(phosphonoacetyl)-dipeptide derivatives and evaluation of their antihypertensive activity.
A series of N-(phosphonoacetyl)-dipeptide derivatives was synthesized for pharmacological testing as antihypertensive compounds. Several of these compounds demonstrated a moderate antihypertensive effect in Wistar spontaneous hypertensive rats (SHR) with p.o. dosing. ACE inhibition by the compounds was studied using ACE from rat plasma and lung. Inhibitors containing esterified C-termini are pro-drugs and showed activity only for plasma ACE.
Osapay
G
G
Research Institute of Chinoin Pharmaceutical and Chemical Works, L Eötvös University, Budapest, Hungary.
Körmöczy
P
P
Szilágyi
I
I
Kajtár
J
J
Kiss
B
B
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis*; D001794:Blood Pressure / Q000187:drug effects; D004151:Dipeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D008168:Lung / Q000201:enzymology; D007703:Peptidyl-Dipeptidase A / Q000378:metabolism; D010746:Phosphonoacetic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D011918:Rats, Inbred SHR; D011919:Rats, Inbred Strains
D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D004151:Dipeptides; D007703:Peptidyl-Dipeptidase A; D010746:Phosphonoacetic Acid