设计、合成及系统评价 4-芳基哌嗪和 4-苄基哌啶萘基醚类单胺类神经递质再摄取抑制剂。
Design, synthesis, and systematic evaluation of 4-arylpiperazine- and 4-benzylpiperidine napthyl ethers as inhibitors of monoamine neurotransmitters reuptake.
机构信息
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 61186, Republic of Korea.
College of Pharmacy and Natural Medicine Research Institute, Mokpo National University, Jeonnam 58554, Republic of Korea.
出版信息
Bioorg Med Chem. 2018 Nov 1;26(20):5538-5546. doi: 10.1016/j.bmc.2018.09.033. Epub 2018 Sep 26.
Two series of 4-arylpiperazine- and 4-benzylpiperidine naphthyl ethers were designed based on structure-activity relationship (SAR) and docking model of reported monoamine neurotransmitters reuptake inhibitors. The compounds were synthesized in 3-simple steps and their biological activities were evaluated. Several compounds were proven to be potent inhibitors of serotonin and norepinephrine reuptake. Computer docking was performed to study the interaction of the most potent compound 35 with human serotonin transporter. The results of the analyses suggest that 4-arylpiperazine- and 4-benzylpiperidine naphthyl ethers might be promising antidepressants worthy of further studies.
基于已报道的单胺类神经递质再摄取抑制剂的结构-活性关系（SAR）和对接模型，设计了两个系列的 4-芳基哌嗪和 4-苄基哌啶萘基醚。这些化合物通过 3 步简单合成法进行合成，并评估了它们的生物活性。一些化合物被证明是强效的 5-羟色胺和去甲肾上腺素再摄取抑制剂。进行了计算机对接研究，以研究最有效的化合物 35 与人类 5-羟色胺转运体的相互作用。分析结果表明，4-芳基哌嗪和 4-苄基哌啶萘基醚可能是有前途的抗抑郁药，值得进一步研究。
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