Zhou D, Stack GP, Lo J, Failli AA, Evrard DA, Harrison BL, Hatzenbuhler NT, Tran M, Croce S, Yi S, Golembieski J, Hornby GA, Lai M, Lin Q, Schechter LE, Smith DL, Shilling AD, Huselton C, Mitchell P, Beyer CE, Andree TH
Synthesis, Potency, and in Vivo Evaluation of 2-Piperazin-1-ylquinoline Analogues as Dual Serotonin Reuptake Inhibitors and Serotonin 5-HT(1A) Receptor Antagonists. [Journal Article]
J Med Chem 2009 Aug 13; 52(15):4955-9.
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-HT(1A) receptor antagonists. In particular, compound 7 exhibits potent functional activities at both the 5-HT transporter and 5-HT(1A) receptor, good selectivity over the alpha(1)-adrenergic and dopaminergic receptors, acceptable pharmacokinetic properties, and a favorable in vivo profile.
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