BENZOFURAN BASED ANGIOTENSIN-II ANTAGONISTS RELATED TO GR117289 .2. AMINO-ACID AMIDES

被引：7

作者：

MIDDLEMISS, D

WATSON, SP

ROSS, BC

DOWLE, MD

SCOPES, DIC

MONTANA, JG

HIRST, GC

PANCHAL, TA

PATON, JMS

HUBBARD, T

STUART, G

DREW, GM

HILDITCH, A

TRAVERS, A

ROBERTSON, MJ

HUNT, AAE

PALMER, E

MANCHEE, GR

机构：

[1] Glaxo Group Research, Ware

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)81011-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of GR117289 derived amino acid-amide angiotensin II antagonists is described. The possibility that the amino acid-amide element of these molecules mimics the C-terminus of Angiotensin II is discounted. One of these compounds, (2g), exhibits good oral activity in the renal hypertensive rat, but has a poor pharmacokinetic profile in the dog.

引用

页码：2043 / 2046

页数：4

共 8 条

[1]

CANGIANO JL, 1979, J PHARMACOL EXP THER, V208, P310

[2] BENZOFURAN BASED ANGIOTENSIN-II ANTAGONISTS RELATED TO GR117289 - ENHANCEMENT OF POTENCY INVITRO AND ORAL ACTIVITY [J].

MIDDLEMISS, D ;

WATSON, SP ;

ROSS, BC ;

DOWLE, MD ;

SCOPES, DIC ;

MONTANA, JG ;

SHAH, P ;

HIRST, GC ;

PANCHAL, TA ;

PATON, JMS ;

PASS, M ;

HUBBARD, T ;

HAMBLETT, J ;

CARDWELL, KS ;

JACK, TI ;

STUART, G ;

COOTE, S ;

BRADSHAW, J ;

DREW, GM ;

HILDITCH, A ;

CLARK, KL ;

ROBERTSON, MJ ;

BAYLISS, MK ;

DONNELLY, M ;

PALMER, E ;

MANCHEE, GRM .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (04) :589-594

[3] BROMOBENZOFURANS - A NEW CLASS OF POTENT, NONPEPTIDE ANTAGONISTS OF ANGIOTENSIN-II [J].

MIDDLEMISS, D ;

DREW, GM ;

ROSS, BC ;

ROBERTSON, MJ ;

SCOPES, DIC ;

DOWLE, MD ;

AKERS, J ;

CARDWELL, K ;

CLARK, KL ;

COOTE, S ;

ELDRED, CD ;

HAMBLETT, J ;

HILDITCH, A ;

HIRST, GC ;

JACK, T ;

MONTANA, J ;

PANCHAL, TA ;

PATON, JMS ;

SHAH, P ;

STUART, G ;

TRAVERS, A .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1991, 1 (12) :711-716

[4]

MIDDLEMISS D, 1993, MAR ACS M DENV

[5]

MIDDLEMISS DS, UNPUB

[6]

SOFER RL, 1989, J CARDIOVASC PHAR S4, V7, pS69

[7] 1-(CARBOXYBENZYL)IMIDAZOLE-5-ACRYLIC ACIDS - POTENT AND SELECTIVE ANGIOTENSIN-II RECEPTOR ANTAGONISTS [J].

WEINSTOCK, J ;

KEENAN, RM ;

SAMANEN, J ;

HEMPEL, J ;

FINKELSTEIN, JA ;

FRANZ, RG ;

GAITANOPOULOS, DE ;

GIRARD, GR ;

GLEASON, JG ;

HILL, DT ;

MORGAN, TM ;

PEISHOFF, CE ;

AIYAR, N ;

BROOKS, DP ;

FREDRICKSON, TA ;

OHLSTEIN, EH ;

RUFFOLO, RR ;

STACK, EJ ;

SULPIZIO, AC ;

WEIDLEY, EF ;

EDWARDS, RM .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (04) :1514-1517

[8] PROXIMAL NEPHRON AND RENAL EFFECTS OF DUP-753, A NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONIST [J].

XIE, MH ;

LIU, FY ;

WONG, PC ;

TIMMERMANS, PBMWM ;

COGAN, MG .

KIDNEY INTERNATIONAL, 1990, 38 (03) :473-479

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