Synthesis and pharmacological screening of new angiotensin converting enzyme inhibitors.
We report the preparation of a series of eight L-alanyl-L-proline derivatives and four L-proline derivatives. Their pharmacological activity as antihypertensive agents was examined with reference to changes in the contractile response to angiotensin I (AI), bradykinine (BK) and angiotensin II (AII). Compounds 1g, 1h and 2c were the most powerful when compared with known angiotensin-converting inhibitors such as captopril and enalapril, and were selected for further pharmacological study.
Gubert
S
S
Centro de Investigacion Grupo Ferrer, Juan de Sada, Barcelona, Spain.
Braso
M A
MA
Sacristán
A
A
Ortiz
J A
JA
D000803:Angiotensin I / Q000494:pharmacology; D000804:Angiotensin II / Q000494:pharmacology; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D001682:Biological Availability; D001794:Blood Pressure / Q000187:drug effects; D001920:Bradykinin / Q000494:pharmacology; D002216:Captopril / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D004656:Enalapril / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains
D000806:Angiotensin-Converting Enzyme Inhibitors; D000804:Angiotensin II; D004656:Enalapril; D000803:Angiotensin I; D002216:Captopril; D001920:Bradykinin