BROMOBENZOFURANS - A NEW CLASS OF POTENT, NONPEPTIDE ANTAGONISTS OF ANGIOTENSIN-II

被引:58
作者
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
机构
[1] Glaxo Group Research, Ware
关键词
D O I
10.1016/S0960-894X(01)81053-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This paper describes the synthesis and pharmacology of a novel series of benzofurans which are antagonists of angiotensin II. One of these, the bromobenzofuran 11b, is a potent (apparent pK(B) = 9.8) and specific antagonist angiotensin II which, after oral administration (10mg/Kg), causes marked and long-lasting (> 24h) falls in blood pressure in renal hypertensive rats.
引用
收藏
页码:711 / 716
页数:6
相关论文
共 23 条
[1]   FUNCTIONAL-GROUP CONTRIBUTIONS TO DRUG RECEPTOR INTERACTIONS [J].
ANDREWS, PR ;
CRAIK, DJ ;
MARTIN, JL .
JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (12) :1648-1657
[2]  
Balkrisna S. B., 1981, TETRAHEDRON, V37, P2091
[3]   NOMENCLATURE FOR ANGIOTENSIN RECEPTORS - A REPORT OF THE NOMENCLATURE-COMMITTEE OF THE COUNCIL-FOR-HIGH-BLOOD-PRESSURE-RESEARCH [J].
BUMPUS, FM ;
CATT, KJ ;
CHIU, AT ;
DEGASPARO, M ;
GOODFRIEND, T ;
HUSAIN, A ;
PEACH, MJ ;
TAYLOR, DG ;
TIMMERMANS, PBMWM .
HYPERTENSION, 1991, 17 (05) :720-721
[4]  
CANGIANO JL, 1979, J PHARMACOL EXP THER, V208, P310
[5]  
CARINI DJ, Patent No. 253310
[6]   [H-3] DUP-753, A HIGHLY POTENT AND SPECIFIC RADIOLIGAND FOR THE ANGIOTENSIN-II-1 RECEPTOR SUBTYPE [J].
CHIU, AT ;
MCCALL, DE ;
ALDRICH, PE ;
TIMMERMANS, PBMWM .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1990, 172 (03) :1195-1202
[7]   DUP-532 - A 2ND GENERATION OF NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS [J].
CHIU, AT ;
CARINI, DJ ;
DUNCIA, JV ;
LEUNG, KH ;
MCCALL, DE ;
PRICE, WA ;
WONG, PC ;
SMITH, RD ;
WEXLER, RR ;
TIMMERMANS, PBMWM ;
CHANG, RSL ;
LOTTI, VJ .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 177 (01) :209-217
[8]  
CHIU AT, 1990, J PHARMACOL EXP THER, V252, P711
[9]   THE DISCOVERY OF POTENT NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - A NEW CLASS OF POTENT ANTIHYPERTENSIVES [J].
DUNCIA, JV ;
CHIU, AT ;
CARINI, DJ ;
GREGORY, GB ;
JOHNSON, AL ;
PRICE, WA ;
WELLS, GJ ;
WONG, PC ;
CALABRESE, JC ;
TIMMERMANS, PBMWM .
JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (05) :1312-1329
[10]  
FURUKAWA Y, 1982, Patent No. 4355040