DUAL INHIBITION OF NEUTRAL ENDOPEPTIDASE AND ANGIOTENSIN-CONVERTING ENZYME BY N-PHOSPHONOMETHYL AND N-CARBOXYALKYL DIPEPTIDES

被引:13
作者
DELOMBAERT, S
TAN, J
STAMFORD, LJ
SAKANE, Y
BERRY, C
GHAI, RD
机构
[1] Research Department, Pharmaceutical Division, CIBA-GEIGY Corporation, Summit
关键词
D O I
10.1016/S0960-894X(01)80703-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Structural modifications have been performed on the selective a-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.
引用
收藏
页码:2715 / 2720
页数:6
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