THE PREPARATION OF (PERFLUOROALKYL)IMIDAZOLES AS NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：19

作者：

CARINI, DJ

CHIU, AT

WONG, PC

JOHNSON, AL

WEXLER, RR

TIMMERMANS, PBMWM

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(00)80688-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of (perfluoroalkyl)imidazoles have been prepared and are potent angiotensin II antagonists. One of these compounds, DuP 532, 4-pentafluoroethyl-2-propyl-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]imidazole-5-carboxylic acid, is a selective antagonist of angiotensin II which causes a marked and long-lasting drop in blood pressure when administered orally to a renal hypertensive rat.

引用

收藏

页码：895 / 898

页数：4

相关论文

共 17 条

[1] A REMARKABLY SIMPLE PREPARATION OF (TRIFLUOROMETHYL)CADMIUM AND (TRIFLUOROMETHYL) ZINC REAGENTS DIRECTLY FROM DIFLUORODIHALOMETHANES [J].

BURTON, DJ ;

WIEMERS, DM .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1985, 107 (17) :5014-5015

[2] 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

[3] NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - N-[(BENZYLOXY)BENZYL]IMIDAZOLES AND RELATED-COMPOUNDS AS POTENT ANTIHYPERTENSIVES [J].

CARINI, DJ ;

DUNCIA, JV ;

JOHNSON, AL ;

CHIU, AT ;

PRICE, WA ;

WONG, PC ;

TIMMERMANS, PBMW .

JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (05) :1330-1336

[4] 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

[5] 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

[6] 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

[7] THE PREPARATION OF F-CADMIUM REAGENTS DIRECTLY FROM F-ALKYL IODIDES AND F-ARYL BROMIDE AND CADMIUM METAL [J].

HEINZE, PL ;

BURTON, DJ .

JOURNAL OF FLUORINE CHEMISTRY, 1985, 29 (03) :359-361

[8]

MARSDEN PA, 1990, HYPERTENSION PATHOPH, P1247

[9] DESIGN OF SPECIFIC INHIBITORS OF ANGIOTENSIN-CONVERTING ENZYME - NEW CLASS OF ORALLY ACTIVE ANTIHYPERTENSIVE AGENTS [J].

ONDETTI, MA ;

CUSHMAN, DW .

SCIENCE, 1977, 196 (4288) :441-444

[10]

PATCHETT AA, 1980, NATURE, V288, P280, DOI 10.1038/288280a0