Synthesis and SAR of 3-and 4-substituted quinolin-2-ones: discovery of mixed 5-HT 1B/5-HT 2A receptor antagonists

…, AM Galzin, M Delahaye, F Guilbert, S O'Connor

Index: 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 Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 8 p. 2129 - 2137

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Citation Number: 19

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 ...