Design and Synthesis of Novel Arylpiperazine Derivatives Containing the Imidazole Core Targeting 5-HT2A Receptor and 5-HT Transporter

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• 作者：Hee Jeong Seo ; Eun-Jung Park ; Min Ju Kim ; Suk Youn Kang ; Suk Ho Lee ; Hyun Jung Kim ; Ki Nam Lee ; Myung Eun Jung ; MinWoo Lee ; Mi-Soon Kim ; Eun-Jung Son ; Woo-Kyu Park ; Jeongmin Kim ; Jinhwa Lee
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：September 22, 2011
• 年：2011
• 卷：54
• 期：18
• 页码：6305-6318
• 全文大小：1196K
• 年卷期：v.54,no.18(September 22, 2011)
• ISSN：1520-4804

文摘

Serotonin antagonist reuptake inhibitor (SARI) drugs that block both 5-HT₂ receptors and the serotonin transporters have been developed. The human 5-HT_2A/2C receptor has been implicated in several neurological conditions, and potent selective 5-HT_2A/2C ligands may have therapeutic potential for treatment of CNS diseases such as depression. An imidazole moiety usually provides good pharmacokinetic properties as a drug substance, and thus considerable efforts have been devoted to develop imidazole derivatives into drug candidates. The imidazole series of compounds was evaluated against 5-HT_2A/2C and serotonin reuptake inhibition. A few of the compounds in the series showed promising IC₅₀ values and antidepressant-like effect in in vivo forced swimming test (FST). On the basis of these results, further lead optimization studies resulted in identifying promising compounds potentially for therapeutic use.