Benzolactams. A new class of converting enzyme inhibitors.
A series of potent inhibitors of angiotensin-converting enzyme (dipeptidyl carboxypeptidase, E.C. 3.4.15.1) derived from benzofused 1-carboxyalkyl-3-(1-carboxy-3-phenyl-propylamino) lactams (III) is described. In the most effective inhibitors (I50 2-4 X 10(-9)M) the lactam is 7 or 8 membered and the N-1 side chain is carboxymethyl or carboxyethyl. Conformational and steric factors pertinent to binding to the enzyme are discussed.
D000806:Angiotensin-Converting Enzyme Inhibitors; D007202:Indicators and Reagents; D007769:Lactams / Q000138:chemical synthesis* / Q000494:pharmacology; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
D000806:Angiotensin-Converting Enzyme Inhibitors; D007202:Indicators and Reagents; D007769:Lactams