NOVEL 1,2,4-OXADIAZOLES AS POTENT AND SELECTIVE HISTAMINE H-3 RECEPTOR ANTAGONISTS

Authors
CLITHEROW JW BESWICK P IRVING WJ SCOPES DIC BARNES JC CLAPHAM J BROWN JD EVANS DJ HAYES AG
Citation
Jw. Clitherow et al., NOVEL 1,2,4-OXADIAZOLES AS POTENT AND SELECTIVE HISTAMINE H-3 RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(7), 1996, pp. 833-838
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
7
Year of publication
1996
Pages
833 - 838
Database
ISI
SICI code
0960-894X(1996)6:7<833:N1APAS>2.0.ZU;2-Q
Abstract
Replacement of the isothiourea moiety of known histamine H-3 antagonis ts by certain 5-membered heteroaromatic systems can give compounds wit h an improved activity profile. One of these, chlorophenyl)methyl]-5-[ 2-(1H-imidazol-4-yl)ethyl] 1,2,4-oxadiazole (GR175737) is a potent, se lective, orally active and centally penetrating H-3 antagonist. Copyri ght (C) 1996 Elsevier Science Ltd