S. Delombaert et al., DUAL INHIBITION OF NEUTRAL ENDOPEPTIDASE AND ANGIOTENSIN-CONVERTING ENZYME BY N-PHOSPHONOMETHYL AND N-CARBOXYALKYL DIPEPTIDES, Bioorganic & medicinal chemistry letters, 4(22), 1994, pp. 2715-2720
Structural modifications have been performed on the selective a-amino
phosphonic acid NEP inhibitor CGS 24592, to achieve dual ACE/NEP inhib
ition in vitro. -Phosphonomethyl-valyl-(S)-(4-phenyl)phenylalanine (19
) is representative of a new type of phosphorus-containing ACE/NEP inh
ibitors, approaching the in vitro potency of the sulfhydryl ACE inhibi
tor captopril and the NEP inhibitor thiorphan.