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Titolo:
5-HT6 receptor antagonists: lead optimisation and biological evaluation ofN-aryl and N-heteroaryl 4-amino-benzene sulfonamides
Autore:
Bos, M; Sleight, AJ; Godel, T; Martin, JR; Riemer, C; Stadler, H;
Indirizzi:
Boehringer Ingelheim Canada Ltd, Res & Dev, Laval, PQ H7S 2G5, Canada Boehringer Ingelheim Canada Ltd Laval PQ Canada H7S 2G5 Q H7S 2G5, Canada Hoffmann La Roche Ag, Div Pharma, Preclin Res, CH-4070 Basel, Switzerland Hoffmann La Roche Ag Basel Switzerland CH-4070 H-4070 Basel, Switzerland
Titolo Testata:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 2, volume: 36, anno: 2001,
pagine: 165 - 178
SICI:
0223-5234(200102)36:2<165:5RALOA>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
CENTRAL-NERVOUS-SYSTEM; MESSENGER-RNA; RAT-BRAIN; SEROTONIN; POTENT; 5-HYDROXYTRYPTAMINE; DERIVATIVES; SB-271046;
Keywords:
sulfonamides; serotonin; passive avoidance paradigm; brain penetration; lipophilicity;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
34
Recensione:
Indirizzi per estratti:
Indirizzo: Bos, M Boehringer Ingelheim Canada Ltd, Res & Dev, 2100 Cunard St, Laval, PQ H7S 2G5, Canada Boehringer Ingelheim Canada Ltd 2100 Cunard St Laval PQ Canada H7S 2G5
Citazione:
M. Bos et al., "5-HT6 receptor antagonists: lead optimisation and biological evaluation ofN-aryl and N-heteroaryl 4-amino-benzene sulfonamides", EUR J MED C, 36(2), 2001, pp. 165-178

Abstract

RO-04-6790 (6a) has been identified in a random screen for 5-HT6 receptor antagonists. In a medicinal chemistry optimisation program a series of analogs comprising N-heteroaryl- and N-arylbenzenesulfonamides have been synthesised and investigated for their binding affinity. Compounds with a log D profile indicative of brain penetration have been subjected to in vivo testing for reversal of a scopolamine-induced retention deficit in a passive avoidance paradigm. (C) 2001 Editions scientifiques et medicales Elsevier SAS.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 07/04/20 alle ore 03:56:35