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Titolo:
Synthesis and SAR of 3-and 4-substituted quinolin-2-ones: Discovery of mixed 5-HT1B/5-HT2A receptor antagonists
Autore:
McCort, G; Hoornaert, C; Aletru, M; Denys, C; Duclos, O; Cadilhac, C; Guilpain, E; Dellac, G; Janiak, P; Galzin, AM; Delahaye, M; Guilbert, F; OConnor, S;
Indirizzi:
Sanofi Synthelabo Rech, Dept Cardiovasc Thrombosis Med Chem, F-91385 Chilly Mazarin, France Sanofi Synthelabo Rech Chilly Mazarin France F-91385 lly Mazarin, France Sanofi Synthelabo Rech, Dept Cardiovasc Thrombosis Pharmacol, F-91385 Chilly Mazarin, France Sanofi Synthelabo Rech Chilly Mazarin France F-91385 lly Mazarin, France
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 8, volume: 9, anno: 2001,
pagine: 2129 - 2137
SICI:
0968-0896(200108)9:8<2129:SASO34>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN CORONARY-ARTERIES; 5-HT1B RECEPTOR; PHARMACOLOGICAL CHARACTERIZATION; SUBCUTANEOUS SUMATRIPTAN; SAPHENOUS-VEIN; MESSENGER-RNA; 5-HYDROXYTRYPTAMINE; SEROTONIN; CONTRACTION; 5-HT1D-BETA;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
37
Recensione:
Indirizzi per estratti:
Indirizzo: McCort, G Sanofi Synthelabo Rech, Dept Cardiovasc Thrombosis Med Chem, 1 Ave Pierre Brossolette, F-91385 Chilly Mazarin, France Sanofi Synthelabo Rech 1 Ave Pierre Brossolette Chilly Mazarin France F-91385
Citazione:
G. McCort et al., "Synthesis and SAR of 3-and 4-substituted quinolin-2-ones: Discovery of mixed 5-HT1B/5-HT2A receptor antagonists", BIO MED CH, 9(8), 2001, pp. 2129-2137

Abstract

Quinolin-2-ones bearing a heteroaryl-piperazine linked by a two carbon chain at the 3- or 4-position were synthesised and evaluated as mixed 5-HT1B/5-HT2A receptor antagonists. Potent mixed antagonists were obtained with thieno[3,2-c]pyridine derivatives. In this series, compound 2.1 (SL 65.0472) proved to be functional antagonist at both the 5-HT2A receptor (rat in vivo 5-HT-induced hypertension model) and the 5-HT1B receptor (dog in vitro saphenous vein assay). (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 15:00:26