IMIDAZOLINONES AS NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：10

作者：

QUAN, ML

DELUCCA, I

BOSWELL, GA

CHIU, AT

WONG, PC

WEXLER, RR

TIMMERMANS, PBMWM

机构：

[1] The DuPont Merck Pharmaceutical Company, Experimental Station, Wilmington, DE 19880-0402

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)80526-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of biphenyl imidazolinones were synthesized as nonpeptide angiotensin II receptor antagonists. While those compounds with a tetrazole functionality were found to be AT(1) selective, those with a sulfonamide moiety showed affinities for both the AT(1) and the AT(2) sites. Representative compounds were very active in lowering blood pressure in conscious renal hypertensive rats following intravenous administration.

引用

页码：1527 / 1530

页数：4

共 13 条

[1] A NEW SERIES OF IMIDAZOLONES - HIGHLY SPECIFIC AND POTENT NONPEPTIDE AT(1) ANGIOTENSIN-II RECEPTOR ANTAGONISTS [J].

BERNHART, CA ;

PERREAUT, PM ;

FERRARI, BP ;

MUNEAUX, YA ;

ASSENS, JLA ;

CLEMENT, J ;

HAUDRICOURT, F ;

MUNEAUX, CF ;

TAILLADES, JE ;

VIGNAL, MA ;

GOUGAT, J ;

GUIRAUDOU, PR ;

LACOUR, CA ;

ROCCON, A ;

CAZAUBON, CF ;

BRELIERE, JC ;

LEFUR, G ;

NISATO, D .

JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (22) :3371-3380

[2]

BRILLA CG, 1992, CIRCULATION, V86, P1

[3]

BUHLMAYER P, 1992, CURRENT OPINION THER, P1693

[4]

CHIU AT, 1990, J PHARMACOL EXP THER, V252, P711

[5] 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

[6]

CHIU AT, 1992, J HYPERTENS, V5, P406

[7] THE DISCOVERY OF DUP-753, A POTENT, ORALLY ACTIVE NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONIST [J].

DUNCIA, JV ;

CARINI, DJ ;

CHIU, AT ;

JOHNSON, AL ;

PRICE, WA ;

WONG, PC ;

WEXLER, RR ;

TIMMERMANS, PBMWM .

MEDICINAL RESEARCH REVIEWS, 1992, 12 (02) :149-191

[8] DEVELOPMENT OF TETRAZOLE BIOISOSTERES IN ANGIOTENSIN-II ANTAGONISTS [J].

FERRARI, B ;

TAILLADES, J ;

PERREAUT, P ;

BERNHART, C ;

GOUGAT, J ;

GUIRAUDOU, P ;

CAZAUBON, C ;

ROCCON, A ;

NISATO, D ;

LEFUR, G ;

BRELIERE, JC .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (01) :45-50

[9] ROLE OF ANGIOTENSIN SUBTYPE-2 RECEPTOR IN NEOINTIMA FORMATION AFTER VASCULAR INJURY [J].

JANIAK, P ;

PILLON, A ;

PROST, JF ;

VILAINE, JP .

HYPERTENSION, 1992, 20 (06) :737-745

[10] POTENT IMIDAZOLE ANGIOTENSIN-II ANTAGONISTS - ACYL SULFONAMIDES AND ACYL SULFAMIDES AS TETRAZOLE REPLACEMENTS [J].

NAYLOR, EM ;

CHAKRAVARTY, PK ;

COSTELLO, CA ;

CHANG, RS ;

CHEN, TB ;

FAUST, KA ;

LOTTI, VJ ;

KIVLIGHN, SD ;

ZINGARO, GJ ;

SIEGL, PKS ;

WONG, PC ;

CARINI, DJ ;

WEXLER, RR ;

PATCHETT, AA ;

GREENLEE, WJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (01) :69-74

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