189003-92-7Relevant articles and documents
Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: Discovery of mixed 5-HT1B/5-HT2A receptor antagonists
McCort, Gary,Hoornaert, Christian,Aletru, Michel,Denys, Colombe,Duclos, Olivier,Cadilhac, Caroline,Guilpain, Eric,Dellac, Genevieve,Janiak, Philip,Galzin, Anne-Marie,Delahaye, Monique,Guilbert, Frederique,O'Connor, Stephen
, p. 2129 - 2137 (2001)
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).
QUINOLEIN-2(1H)-ONE DERIVATIVES AS SEROTONIN ANTAGONISTS
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, (2008/06/13)
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