Novel 1,2,4-oxadiazoles as potent and selective histamine H-3 receptor antagonists

被引：98

作者：

Clitherow, JW ^{[1
]}

Beswick, P ^{[1
]}

Irving, WJ ^{[1
]}

Scopes, DIC ^{[1
]}

Barnes, JC ^{[1
]}

Clapham, J ^{[1
]}

Brown, JD ^{[1
]}

Evans, DJ ^{[1
]}

Hayes, AG ^{[1
]}

机构：

[1] GLAXO WELLCOME MED RES CTR,DEPT PHARMACOL,STEVENAGE SG1 2NY,HERTS,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 07期

关键词：

D O I：

10.1016/0960-894X(96)00122-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Replacement of the isothiourea moiety of known histamine H-3 antagonists by certain 5-membered heteroaromatic systems can give compounds with an improved activity profile. One of these, 3-[(4-chlorophenyl)methyl]-5-[2-(1H-imidazol-4-yl)ethyl] 1,2,4-oxadiazole (GR175737) is a potent, selective, orally active and centally penetrating H-3 antagonist. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：833 / 838

页数：6

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