Design and synthesis of novel tricyclic benzoxazines as potent 5-HT 1A/B/D receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4 h-imidazo[5,1-c][1,4] benzoxazine-3-carboxamide (GSK588045)

Journal of Medicinal Chemistry

Volumn 53, Issue 15, 2010, Pages 5827-5843

  Bromidge, Steven M ^a   Arban, Roberto ^b   Bertani, Barbara ^b   Bison, Silvia ^b   Borriello, Manuela ^b   Cavanni, Paolo ^b   Dal Forno, Giovanna ^b   Di Fabio, Romano ^b   Donati, Daniele ^b   Fontana, Stefano ^b   Gianotti, Massimo ^b   Gordon, Laurie J ^a   Granci, Enrica ^b   Leslie, Colin P ^b   Moccia, Luca ^b   Pasquarello, Alessandra ^b   Sartori, Ilaria ^b   Sava, Anna ^b   Watson, Jeannette M ^a   Worby, Angela ^a   Zonzini, Laura ^b   Zucchelli, Valeria ^b   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b Medicines Research Centre   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

6 [2 [4 (2 METHYL 5 QUINOLINYL) 1 PIPERAZINYL]ETHYL] 4H IMIDAZO[5,1 C][1,4]BENZOXAZINE 3 CARBOXAMIDE; ATORVASTATIN; BENZOXAZINE DERIVATIVE; GSK 588045; MIDAZOLAM; NIFEDIPINE; POTASSIUM CHANNEL HERG; SEROTONIN 1A ANTAGONIST; SEROTONIN 1B ANTAGONIST; SEROTONIN 1D ANTAGONIST; UNCLASSIFIED DRUG;

ARTICLE; DRUG ACTIVITY; DRUG DESIGN; DRUG INHIBITION; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; NONHUMAN; PHARMACODYNAMICS;

ANIMALS; ANTI-ANXIETY AGENTS; ANTIDEPRESSIVE AGENTS; BENZOXAZINES; CALLITHRIX; CELL LINE; CEREBRAL CORTEX; CRICETINAE; CRICETULUS; CYTOCHROME P-450 ENZYME SYSTEM; ETHER-A-GO-GO POTASSIUM CHANNELS; GUINEA PIGS; HUMANS; MALE; MICROSOMES, LIVER; PROTEIN BINDING; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTOR, SEROTONIN, 5-HT1A; RECEPTOR, SEROTONIN, 5-HT1B; RECEPTOR, SEROTONIN, 5-HT1D; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77955403136     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100482n     Document Type: Article

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