A NEW CLASS OF DIACIDIC NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：14

作者：

CHO, N ^{[1
]}

KUBO, K ^{[1
]}

FURUYA, S ^{[1
]}

SUGIURA, Y ^{[1
]}

YASUMA, T ^{[1
]}

KOHARA, Y ^{[1
]}

OJIMA, M ^{[1
]}

INADA, Y ^{[1
]}

NISHIKAWA, K ^{[1
]}

NAKA, T ^{[1
]}

机构：

[1] TAKEDA CHEM IND LTD, PHARMACEUT RES LABS, YODOGAWA KU, OSAKA, JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)81118-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of heterocyclic compounds I bearing two acidic functionalities, a carboxyl group and a tetrazole ring, was prepared and evaluated for in vitro and in vivo angiotensin II (AII) antagonistic activity. These compounds showed significantly more potent AII antagonistic activities than the parent compounds without the carboxyl groups. This structure-activity relationship (SAR) study revealed the importance of the carboxyl group attached to the heterocyclic moieties especially for insurmountable antagonism and enhancement of in vivo (po) activity.

引用

页码：35 / 40

页数：6

共 50 条

[31] A NEW SERIES OF IMIDAZOLONES - HIGHLY SPECIFIC AND POTENT NONPEPTIDE AT(1) ANGIOTENSIN-II RECEPTOR ANTAGONISTS
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
[32] NONPEPTIDE ANGIOTENSIN-II (AII) RECEPTOR ANTAGONISTS - STUDIES WITH EXP9270
WONG, PC
PRICE, WA
CHIU, AT
CARINI, DJ
DUNCIA, JV
JOHNSON, AL
WEXLER, RR
TABER, RI
TIMMERMANS, PBMWM
HYPERTENSION, 1989, 14 (03) : 348 - 348
[33] ANGIOTENSIN-II RECEPTORS AND ANGIOTENSIN-II RECEPTOR ANTAGONISTS
TIMMERMANS, PBMWM
WONG, PC
CHIU, AT
HERBLIN, WF
BENFIELD, P
CARINI, DJ
LEE, RJ
WEXLER, RR
SAYE, JAM
SMITH, RD
PHARMACOLOGICAL REVIEWS, 1993, 45 (02) : 205 - 251
[34] NONPEPTIDE ANGIOTENSIN-II (AII) RECEPTOR ANTAGONISTS - PHARMACOLOGY OF DUP-532
WONG, PC
CARINI, DJ
CHIU, AT
HART, SD
PRICE, WA
WEXLER, RR
SMITH, RD
TIMMERMANS, PBMWM
FASEB JOURNAL, 1991, 5 (05): : A1039 - A1039
[35] NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - SYNTHESIS AND BIOLOGICAL-ACTIVITY OF BENZIMIDAZOLES
KUBO, K
INADA, Y
KOHARA, Y
SUGIURA, Y
OJIMA, M
ITOH, K
FURUKAWA, Y
NISHIKAWA, K
NAKA, T
JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (12) : 1772 - 1784
[36] GLOMERULAR EFFECTS OF ANGIOTENSIN-II - A REAPPRAISAL BASED ON STUDIES WITH NONPEPTIDE RECEPTOR ANTAGONISTS
ARDAILLOU, R
CHANSEL, D
JOURNAL OF HYPERTENSION, 1993, 11 : S43 - S47
[37] NONPEPTIDE ANTAGONISTS OF ANGIOTENSIN-II - IMIDAZOPYRIDYL-BROMOBENZOFURANS
JUDD, DB
CARDWELL, KS
PANCHAL, TA
JACK, TI
PASS, M
HUBBARD, T
DEAN, AW
CURRIE, GS
MIDDLEMISS, D
ALLEN, D
DREW, GM
HILDITCH, A
GALLACHER, D
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1993, 206 : 84 - MEDI
[38] Discovery of a new class of antihypertensive agents, nonpeptide angiotensin II receptor antagonists : Candesartan cilexetil
Naka, T
NIPPON NOGEIKAGAKU KAISHI-JOURNAL OF THE JAPAN SOCIETY FOR BIOSCIENCE BIOTECHNOLOGY AND AGROCHEMISTRY, 2000, 74 (07): : 787 - 790
[39] ANGIOTENSIN-II RECEPTOR ANTAGONISTS
VANMEEL, JCA
ENTZEROTH, M
HAUEL, N
NARR, B
RIES, U
WIENEN, W
ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH, 1993, 43-1 (2A): : 242 - 246
[40] Angiotensin-II receptor antagonists
Chung, O
Unger, T
INTERNIST, 1996, 37 (05): : 534 - 538

← 1 2 3 4 5 →