| 11504649 |
McCort G, Hoornaert C, Aletru M, Denys C, Duclos O, Cadilhac C, Guilpain E, Dellac G, Janiak P, Galzin AM, Delahaye M, Guilbert F, O'Connor S: Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: discovery of mixed 5-HT (1B)/5-HT (2A) receptor antagonists. Bioorg Med Chem. 2001 Aug;9(8):2129-37.
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-HT (1B)/5-HT (2A) 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-HT (2A) receptor (rat in vivo 5-HT-induced hypertension model) and the 5-HT (1B) receptor (dog in vitro saphenous vein assay). |
83(1,1,1,3) |