MERCAPTOACYL DIPEPTIDES AS DUAL INHIBITORS OF ANGIOTENSIN-CONVERTING ENZYME AND NEUTRAL ENDOPEPTIDASE - PRELIMINARY STRUCTURE-ACTIVITY STUDIES

被引:36
作者
DELANEY, NG [1 ]
BARRISH, JC [1 ]
NEUBECK, R [1 ]
NATARAJAN, S [1 ]
COHEN, M [1 ]
ROVNYAK, GC [1 ]
HUBER, G [1 ]
MURUGESAN, N [1 ]
GIROTRA, R [1 ]
SIEBERMCMASTER, E [1 ]
ROBL, JA [1 ]
ASAAD, MM [1 ]
CHEUNG, HS [1 ]
BIRD, JE [1 ]
WALDRON, T [1 ]
PETRILLO, EW [1 ]
机构
[1] BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,PRINCETON,NJ 08543
关键词
D O I
10.1016/S0960-894X(01)80371-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Mercaptoacyl dipeptides were prepared as dual-acting ACE/NEP inhibitors. Inhibition of each enzyme may be explained by different binding models. Structure-activity studies determined that, in this series of compounds, the mercaptopropanoyl dipeptide framework leads to increased affinity for NEP but diminished ACE activity in vivo.
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页码:1783 / 1788
页数:6
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