A new class of angiotensin-converting enzyme inhibitors.
Much current attention focuses on the renin-angiotensin system in relation to mechanisms controlling blood pressure and renal function. Recent demonstrations (ref. 1, ref. 2 and refs therein) that angiotensin-converting enzyme inhibitors show promising clinical antihypertensive properties have been of particular interest. We now report on the design of a novel series of substituted N-carboxymethyl-dipeptides which are active in inhibiting angiotensin-converting enzyme at nanomolar levels. We suggest that these compounds are transition-state inhibitors and that extensions of this design to other metalloendopeptidases merit further study.
D000806:Angiotensin-Converting Enzyme Inhibitors; D000818:Animals; D001665:Binding Sites; D004151:Dipeptides / Q000494:pharmacology; D004285:Dogs; D008667:Metalloproteins / Q000037:antagonists & inhibitors; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000806:Angiotensin-Converting Enzyme Inhibitors; D004151:Dipeptides; D008667:Metalloproteins