Dipeptide mimics. Conformationally restricted inhibitors of angiotensin-converting enzyme

A series of potent inhibitors of angiotensin-converting enzyme (dipeptidyl carboxy-peptidase, E.C. 3.4.15.1) is described which addresses conformational aspects of the enzyme-inhibitor interaction. Conformational probes were derived from simple lactams containing the required recognition and binding...

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Veröffentlicht in:Biochemical and biophysical research communications 1983-02, Vol.111 (1), p.166-171
Hauptverfasser: Thorsett, E.D., Harris, E.E., Aster, S., Peterson, E.R., Taub, D., Patchett, A.A., Ulm, E.H., Vassil, T.C.
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Sprache:eng
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Zusammenfassung:A series of potent inhibitors of angiotensin-converting enzyme (dipeptidyl carboxy-peptidase, E.C. 3.4.15.1) is described which addresses conformational aspects of the enzyme-inhibitor interaction. Conformational probes were derived from simple lactams containing the required recognition and binding elements. The inhibitor potencies vary with lactam ring size in a manner predicted from molecular modeling studies and help map the active site of this important enzyme.
ISSN:0006-291X
1090-2104
DOI:10.1016/S0006-291X(83)80131-4