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. 1980 Nov 20;288(5788):280-3.
doi: 10.1038/288280a0.

A new class of angiotensin-converting enzyme inhibitors

A A Patchett, E Harris, E W Tristram, M J Wyvratt, M T Wu, D Taub, E R Peterson, T J Ikeler, J ten Broeke, L G Payne, D L Ondeyka, E D Thorsett, W J Greenlee, N S Lohr, R D Hoffsommer, H Joshua, W V Ruyle, J W Rothrock, S D Aster, A L Maycock, F M Robinson, R Hirschmann, C S Sweet, E H Ulm, D M Gross, T C Vassil, C A Stone

A new class of angiotensin-converting enzyme inhibitors

A A Patchett et al. Nature. .

Abstract

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.

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