Zhou, Dahui; Zhou, Ping; Evrard, Deborah A.; Meagher, Kristin; Webb, Michael; Harrison, Boyd L.; Huryn, Donna M.; Golembieski, Jeannette; Hornby, Geoffrey A.; Schechter, Lee E.; Smith, Deborah L.; Andree, Terrance H.; Mewshaw, Richard E. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Studies toward the discovery of the next generation of antidepressants. Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives》.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole The author mentioned the following in the article:
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-HT1A 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 (I) exhibited equal binding affinities at 5-HT transporter (Ki = 4.9 nM), 5-HT1A receptor (Ki = 6.2 nM) and functioned as a 5-HT1A receptor antagonist. The experimental part of the paper was very detailed, including the reaction process of 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole)
4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Application In Synthesis of 4-(Piperazin-1-yl)-1H-indole
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics