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

McCort, G; Hoornaert, C; Aletru, M; Denys, C; Duclos, O; Cadilhac, C; Guilpain, E; Dellac, G; Janiak, P; Galzin, A M; Delahaye, M; Guilbert, F; O'Connor, S.

Bioorg Med Chem ; 9(8): 2129-37, 2001 Aug.

Article in English | MEDLINE | ID: mdl-11504649

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-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).

Subject(s)

Piperazines/chemical synthesis , Quinolines/chemical synthesis , Receptors, Serotonin/metabolism , Serotonin Antagonists/chemical synthesis , Animals , Dogs , Piperazines/chemistry , Piperazines/pharmacology , Quinolines/chemistry , Quinolines/pharmacology , Rats , Receptor, Serotonin, 5-HT1B , Receptor, Serotonin, 5-HT2A , Receptors, Serotonin/drug effects , Serotonin Antagonists/chemistry , Serotonin Antagonists/pharmacology

ABSTRACT

Subject(s)

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