Title of article :
Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: discovery of mixed 5-HT1B/5-HT2A receptor antagonists Original Research Article
Author/Authors :
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، نويسنده , , 2-c]pyridine derivatives. In this series، نويسنده , , 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).، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2001
Abstract :
Gary McCort, Christian Hoornaert, Michel Aletru, Colombe Denys, Olivier Duclos, Caroline Cadilhac, Eric Guilpain, Geneviève Dellac, Philip Janiak, Anne-Marie Galzin, Monique Delahaye, Frédérique Guilbert, Stephen OʹConnor
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry