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Dual inhibition of neutral endopeptidase and angiotensin-converting enzyme by N-phosphonomethyl and N-carboxyalkyl dipeptides

1994; Elsevier BV; Volume: 4; Issue: 22 Linguagem: Inglês

10.1016/s0960-894x(01)80703-4

1464-3405

Stéphane De Lombaert, Jenny Tan, Lisa J. Stamford, Yumi Sakane, Carol Berry, Rajendra D. Ghai,

Chemical Synthesis and Analysis

Structural modifications have been performed on the selective α-amino phosphonic acid NEP inhibitor CGS 24592, to achieve dual ACE/NEP inhibition in vitro. (S)-N-Phosphonomethyl-valyl-(S)-(4-phenyl)phenylalanine (19) is representative of a new type of phosphorus-containing ACE/NEP inhibitors, approaching the in vitro potency of the sulfhydryl ACE inhibitor captopril and the NEP inhibitor thiorphan.