Ketomethylureas. A New Class of Angiotensin Converting Enzyme Inhibitors

S. Natarajan The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

E. M. Gordon The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

E. F. Sabo The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

J. D. Godfrey The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

H. N. Weller The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

Jelka Pluscec The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

M. B. Rom The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

J. Engebrecht The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

D. W. Cushman The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

J. M. Deforrest The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

J. Powell The Squibb Institute for Medical Research, P.O. Box 4000, Princeton, New Jersey, 08540, USA

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Abstract

The design rationale for a new series of tripeptide derived angiotensin converting enzyme (ACE) inhibitors, which we term “ketomethylureas”, is described. Analogs of tripeptide substrates (i.e. N-benzoyl-Phe-Ala-Pro) in which the nitrogen atom of the scissile amide bond and the adjacent asymmetric carbon atom of the penultimate amino acid residue are formally transposed give rise to this novel class of inhibitors. The most potent ketomethylureas inhibit ACE wtih I₅₀ values in the nM range.

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Ketomethylureas. A New Class of Angiotensin Converting Enzyme Inhibitors

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Ketomethylureas. A New Class of Angiotensin Converting Enzyme Inhibitors

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