Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists

…, S Croce, S Yi, J Golembieski, GA Hornby…

Index: Zhou, Dahui; Stack, Gary P.; Lo, Jennifer; Failli, Amedeo A.; Evrard, Deborah A.; Harrison, Boyd L.; Hatzenbuhler, Nicole T.; Tran, Megan; Croce, Susan; Yi, Soo; Golembieski, Jeannette; Hornby, Geoffrey A.; Lai, Margaret; Lin, Qian; Schechter, Lee E.; Smith, Deborah L.; Shilling, Adam D.; Huselton, Christine; Mitchell, Paul; Beyer, Chad E.; Andree, Terrance H. Journal of Medicinal Chemistry, 2009 , vol. 52, # 15 p. 4955 - 4959

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Citation Number: 10

Abstract

On the basis of the previously reported clinical candidate, SSA-426 (1), a series of related 2- piperazin-1-ylquinoline derivatives 3− 16 were synthesized and evaluated as dual-acting serotonin (5-HT) reuptake inhibitors and 5-HT1A receptor antagonists. In particular, compound 7 exhibits potent functional activities at both the 5-HT transporter and 5-HT1A receptor, good selectivity over the α1-adrenergic and dopaminergic receptors, acceptable ...