SUBSTITUTED PYRROLIDIN-2-ONE BIPHENYLTETRAZOLES AS ANGIOTENSIN-II ANTAGONISTS

被引：13

作者：

MURRAY, WV

LALAN, P

GILL, A

ADDO, MF

LEWIS, JM

LEE, DKH

WACHTER, MP

RAMPULLA, R

UNDERWOOD, DC

机构：

[1] The R.W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, P.O. Box 300

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)80914-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of substituted pyrrolidin-2-ones has been identified as antagonists of the angiotensin II receptor. They are potent inhibitors of angiotensin II induced contractions in rabbit aortic rings, with pA2 values as high as 9. A number of these compounds have been tested in rabbit adrenal cortex binding assays and exhibited IC50's as low as 60nM. Compounds 1e, 1f and 29 have been found to be orally active as anti-hypertensives in spontaneously hypertensive rat preparations.

引用

页码：369 / 374

页数：6

共 20 条

[1] ON THE REGIOSELECTIVITY OF THE CONDENSATION OF STABILIZED PHOSPHOYLIDS WITH 3-SUBSTITUTED PHTHALIC ANHYDRIDES [J].

BREAU, L ;

KAYSER, MM .

CANADIAN JOURNAL OF CHEMISTRY-REVUE CANADIENNE DE CHIMIE, 1989, 67 (04) :569-573

[2] GEOMETRICAL REACTION COORDINATES .2. NUCLEOPHILIC ADDITION TO A CARBONYL GROUP [J].

BURGI, HB ;

DUNITZ, JD ;

SHEFTER, E .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1973, 95 (15) :5065-5067

[3] NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - THE DISCOVERY OF A SERIES OF N-(BIPHENYLYLMETHYL)IMIDAZOLES AS POTENT, ORALLY ACTIVE ANTIHYPERTENSIVES [J].

CARINI, DJ ;

DUNCIA, JV ;

ALDRICH, PE ;

CHIU, AT ;

JOHNSON, AL ;

PIERCE, ME ;

PRICE, WA ;

SANTELLA, JB ;

WELLS, GJ ;

WEXLER, RR ;

WONG, PC ;

YOO, SE ;

TIMMERMANS, PBMWM .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (08) :2525-2547

[4] IDENTIFICATION OF ANGIOTENSIN-II RECEPTOR SUBTYPES [J].

CHIU, AT ;

HERBLIN, WF ;

MCCALL, DE ;

ARDECKY, RJ ;

CARINI, DJ ;

DUNCIA, JV ;

PEASE, LJ ;

WONG, PC ;

WEXLER, RR ;

JOHNSON, AL ;

TIMMERMANS, PBMWM .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1989, 165 (01) :196-203

[5]

CHIU AT, 1990, J PHARMACOL EXP THER, V252, P726

[6] 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

[7] ON THE REGIOSELECTIVITY OF WITTIG REACTIONS WITH UNSYMMETRICALLY SUBSTITUTED SUCCINIC ANHYDRIDES [J].

KAYSER, MM ;

BREAU, L .

CANADIAN JOURNAL OF CHEMISTRY-REVUE CANADIENNE DE CHIMIE, 1989, 67 (09) :1401-1410

[8] EVIDENCE THAT THE APPARENT COMPLEXITY OF RECEPTOR ANTAGONISM BY ANGIOTENSIN-II ANALOGS IS DUE TO A REVERSIBLE AND SYNOPTIC ACTION [J].

LIU, YJ ;

SHANKLEY, NP ;

WELSH, NJ ;

BLACK, JW .

BRITISH JOURNAL OF PHARMACOLOGY, 1992, 106 (02) :233-241

[9] POTENT, ORALLY ACTIVE IMIDAZO[4,5-B]PYRIDINE-BASED ANGIOTENSIN-II RECEPTOR ANTAGONISTS [J].

MANTLO, NB ;

CHAKRAVARTY, PK ;

ONDEYKA, DL ;

SIEGL, PKS ;

CHANG, RS ;

LOTTI, VJ ;

FAUST, KA ;

CHEN, TB ;

SCHORN, TW ;

SWEET, CS ;

EMMERT, SE ;

PATCHETT, AA ;

GREENLEE, WJ .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (09) :2919-2922

[10] 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

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