VALSARTAN, A POTENT, ORALLY-ACTIVE ANGIOTENSIN-II ANTAGONIST DEVELOPED FROM THE STRUCTURALLY NEW AMINO-ACID SERIES

被引：83

作者：

BUHLMAYER, P

FURET, P

CRISCIONE, L

DEGASPARO, M

WHITEBREAD, S

SCHMIDLIN, T

LATTMANN, R

WOOD, J

机构：

[1] Research Department, Pharmaceuticals Division Ciba-Geigy Ltd., CH-4002 Basel, P.O. Box

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)81117-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Starting from the structure of DuP-753 and a 3-dimensional model of the pentapeptide Tyr-Ile-His-Pro-Ile, a series of new and highly potent antagonists has been designed where the imidazole moiety of the Du Pont compound has been-replaced by an N-acylated aminoacid residue. VALSARTAN (Ex. 4e, CGP48933, (S)-N-Valeryl-N-{[2'-(1H-tetrazol-5-yl-)biphenyl-4-yl]methyl}-valine), has been selected for clinical investigation.

引用

页码：29 / 34

页数：6

共 17 条

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