Novel peptides with orally active and long-lasting antihypertensive activity.
A series of N-(P-substituted phosphinoyl)peptides were synthesized and their antihypertensive activities were tested in spontaneously hypertensive rats (SHR). Among them, N-(dibenzyloxyphosphinoyl)-L-Ala-L-Pro-L-Pro-OH showed the most potent and long-lasting antihypertensive activity in SHR when administered orally. Although the inhibitory activity of this peptide against the angiotensin-converting enzyme was about one-hundredth of that of Captopril, the antihypertensive activity in SHR was significantly higher and longer-lasting than that of Enalapril which has been reported to be the most potent agent among similar converting enzyme inhibitors.
D000806:Angiotensin-Converting Enzyme Inhibitors; D000818:Animals; D000959:Antihypertensive Agents / Q000627:therapeutic use*; D001794:Blood Pressure / Q000187:drug effects; D006973:Hypertension / Q000188:drug therapy*; D008297:Male; D010750:Phosphoproteins / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D017976:Phosphorus Acids / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D010750:Phosphoproteins; D017976:Phosphorus Acids