Identification of a novel, orally bioavailable histamine H3 receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template

被引：27

作者：

Aslanian, R ^{[1
]}

Mutahi, MW ^{[1
]}

Shih, NY ^{[1
]}

McCormick, KD ^{[1
]}

Piwinski, JJ ^{[1
]}

Ting, PC ^{[1
]}

Albanese, MM ^{[1
]}

Berlin, MY ^{[1
]}

Zhu, XH ^{[1
]}

Wong, SC ^{[1
]}

Rosenblum, SB ^{[1
]}

Jiang, YH ^{[1
]}

West, R ^{[1
]}

She, S ^{[1
]}

Williams, SM ^{[1
]}

Bryant, M ^{[1
]}

Hey, JA ^{[1
]}

机构：

[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(02)00055-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of histamine H-3 receptor antagonists, based on the 4-benzyl-(1H-imidazole-4-yl) template, incorporating urea and carbamate linkers has been prepared. Compound 3j is a selective H-3 antagonist and demonstrates excellent oral plasma levels in the rat and monkey. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：937 / 941

页数：5

共 19 条

[1] 4-[(1H-imidazol-4-yl)methyl]benzamidines and benzylamidines:: Novel antagonists of the histamine H3 receptor [J].

Aslanian, R ;

Brown, JE ;

Shih, NY ;

Mutahi, MW ;

Green, MJ ;

She, S ;

Del Prado, M ;

West, R ;

Hey, J .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (16) :2263-2268

[2]

ASLANIAN RG, Patent No. 5578616

[3]

ASLANIAN RG, Patent No. 5990147

[4] Development of a pharmacophore model for histamine H3 receptor antagonists, using the newly developed molecular modeling program SLATE [J].

De Esch, IJP ;

Mills, JEJ ;

Perkins, TDJ ;

Romeo, G ;

Hoffmann, M ;

Wieland, K ;

Leurs, R ;

Menge, WMPB ;

Nederkoorn, PHJ ;

Dean, PM ;

Timmerman, H .

JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (11) :1666-1674

[5]

de Esch IJP, 2000, ARCH PHARM, V333, P254

[6]

Galant SP, 1999, FORMULARY, V34, P1016

[7]

Ganellin CR, 1998, ARCH PHARM, V331, P395, DOI 10.1002/(SICI)1521-4184(199812)331:12<395::AID-ARDP395>3.0.CO

[8]

2-7

[9] INHIBITION OF SYMPATHETIC HYPERTENSIVE RESPONSES IN THE GUINEA-PIG BY PREJUNCTIONAL HISTAMINE H3-RECEPTORS [J].

HEY, JA ;

DELPRADO, M ;

EGAN, RW ;

KREUTNER, W ;

CHAPMAN, RW .

BRITISH JOURNAL OF PHARMACOLOGY, 1992, 107 (02) :347-351

[10] CHARACTERIZATION AND TISSUE DISTRIBUTION OF H-3 HISTAMINE-RECEPTORS IN GUINEA-PIGS BY N-ALPHA-METHYLHISTAMINE [J].

KORTE, A ;

MYERS, J ;

SHIH, NY ;

EGAN, RW ;

CLARK, MA .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1990, 168 (03) :979-986

← 1 2 →