Biphenylsulfonamide endothelin receptor antagonists.: Part 3:: Structure-activity relationship of 4′-heterocyclic biphenylsulfonamides

被引：6

作者：

Murugesan, N ^{[1
]}

Gu, ZX ^{[1
]}

Stein, PD ^{[1
]}

Spergel, S ^{[1
]}

Bisaha, S ^{[1
]}

Liu, ECK ^{[1
]}

Zhang, RG ^{[1
]}

Webb, ML ^{[1
]}

Moreland, S ^{[1
]}

Barrish, JC ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Chem, Cardiovasc Agents, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)00791-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A number of 4'-heterocyclic biphenylsulfonamide derivatives, formally derived from BMS-193884 (1) by replacing the oxazole ring with other heterocyclic rings, are potent and selective endothelin A (ETA) receptor antagonists. Among the analogues examined, the pyrimidine derivative 18 is the most potent (K-i = 0.9 nM) and selective for the ETA receptor, approximately equivalent to 1. (C) 2002 Bristol-Myers Squibb Company. Published by Elsevier Science Ltd. All rights reserved.

引用

页码：517 / 520

页数：4

共 15 条

[1]

Brunner Hans R., 1998, American Journal of Hypertension, V11, p103S, DOI 10.1016/S0895-7061(98)00007-7

[2] THE HUMAN ENDOTHELIN FAMILY - 3 STRUCTURALLY AND PHARMACOLOGICALLY DISTINCT ISOPEPTIDES PREDICTED BY 3 SEPARATE GENES [J].

INOUE, A ;

YANAGISAWA, M ;

KIMURA, S ;

KASUYA, Y ;

MIYAUCHI, T ;

GOTO, K ;

MASAKI, T .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1989, 86 (08) :2863-2867

[3]

Love MP, 1996, BASIC RES CARDIOL, V91, P21

[4] Biphenylsulfonamide endothelin antagonists:: Structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2′-amino-N-(3,4-dimethyl-5-isoxazolyl)-4′-(2-methylpropyl)[1,1′-biphenyl]-2-sulfonamide (BMS-187308) [J].

Murugesan, N ;

Gu, ZX ;

Stein, PD ;

Bisaha, S ;

Spergel, S ;

Girotra, R ;

Lee, VG ;

Lloyd, J ;

Misra, RN ;

Schmidt, J ;

Mathur, A ;

Stratton, L ;

Kelly, YF ;

Bird, E ;

Waldron, T ;

Liu, ECK ;

Zhang, RG ;

Lee, H ;

Serafino, R ;

Abboa-Offei, B ;

Mathers, P ;

Giancarli, M ;

Seymour, AA ;

Webb, ML ;

Moreland, S ;

Barrish, JC ;

Hunt, JT .

JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (26) :5198-5218

[5] Biphenylsulfonamide endothelin receptor antagonists.: 2.: Discovery of 4′-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ETA antagonists [J].

Murugesan, N ;

Gu, ZX ;

Stein, PD ;

Spergel, S ;

Mathur, A ;

Leith, L ;

Liu, ECK ;

Zhang, RA ;

Bird, E ;

Waldron, T ;

Marino, A ;

Morrison, RA ;

Webb, ML ;

Moreland, S ;

Barrish, JC .

JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (16) :3111-3117

[6]

MURUGESAN N, 1997, Patent No. 5612359

[7]

MURUGESAN N, 1998, Patent No. 5780473

[8]

Nguyen BNT, 1998, PHARMACOTHERAPY, V18, P706

[9]

Ohlstein EH, 1996, MED RES REV, V16, P365, DOI 10.1002/(SICI)1098-1128(199607)16:4<365::AID-MED4>3.0.CO

[10]

2-V

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