Literature

Abstract

Based on the previously reported discovery lead, 3-(cis-4-(4-(1H-indol-4-yl)piperazin-1-yl)cyclohexyl)-5-fluoro-1H-indole (2), a series of related arylpiperazin-4-yl-cyclohexyl indole analogs were synthesized then evaluated as 5-HT transporter inhibitors and 5-HT(1A) receptor antagonists. The investigation of the structure-activity relationships revealed the optimal pharmacophoric elements required for activities in this series. The best example from this study, 5-(piperazin-1-yl)quinoline analog (trans-20), exhibited equal binding affinities at 5-HT transporter (K(i)=4.9nM), 5-HT(1A) receptor (K(i)=6.2nM) and functioned as a 5-HT(1A) receptor antagonist.

DOI： 10.1016/j.bmc.2008.05.075

Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives

Bioorganic & Medicinal Chemistry 2008.0

Studies toward the Discovery of the Next Generation of Antidepressants. 3. Dual 5-HT1Aand Serotonin Transporter Affinity within a Class ofN-Aryloxyethylindolylalkylamines

Journal of Medicinal Chemistry 2004.0

Advances toward New Antidepressants with Dual Serotonin Transporter and 5-HT1AReceptor Affinity within a Class of 3-Aminochroman Derivatives. Part 2

Journal of Medicinal Chemistry 2008.0

Synthesis, docking and pharmacological evaluation of novel homo- and hetero-bis 3-piperazinylpropylindole derivatives at SERT and 5-HT1A receptor

Bioorganic & Medicinal Chemistry 2013.0

New 1-Aryl-3-(4-arylpiperazin-1-yl)propane Derivatives, with Dual Action at 5-HT1ASerotonin Receptors and Serotonin Transporter, as a New Class of Antidepressants

Journal of Medicinal Chemistry 2001.0

Synthesis, Potency, and in Vivo Evaluation of 2-Piperazin-1-ylquinoline Analogues as Dual Serotonin Reuptake Inhibitors and Serotonin 5-HT1AReceptor Antagonists