Identification of 1-phenoxy-3-(piperazin-1-yl)propan-2-ol derivatives as novel triple reuptake inhibitors,Bulletin of the Korean Chemical Society

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Identification of 1-phenoxy-3-(piperazin-1-yl)propan-2-ol derivatives as novel triple reuptake inhibitors
Bulletin of the Korean Chemical Society ( IF 2.3 ) Pub Date : 2023-03-29 , DOI: 10.1002/bkcs.12693
Md. Ashrafuzzaman _{1,

2} , Su Hyun Ji _{1,

3} , Hyomin Ahn _{1,

4} , Hwan Won Chung ₅ , Daeun Choi ₁ , Ju Jin Park ₁ , Minji Go ₁ , Jung In Pyo ₁ , Azam Sharif Mohammed Shafioul ₁ , Duck‐Hyung Lee ₃ , Sung‐Gil Chi ₄ , Chiman Song ₁ , Chan Seong Cheong ₁ , Seo‐Jung Han _{1,

2}

Affiliation

Novel 1-phenoxy-3-(piperazin-1-yl)propan-2-ol derivatives were designed and synthesized as potential triple reuptake inhibitors, which simultaneously inhibit serotonin, norepinephrine, and dopamine transporters (SERT, NET, and DAT, respectively). Through neurotransmitter transporter uptake assays, inhibitory activities of 1-phenoxy-3-(piperazin-1-yl)propan-2-ol derivatives were evaluated. We discovered compound 19 exhibited the most potent inhibitory activities against all three monoamine neurotransmitter transporters and the IC₅₀ values of 19 against SERT, NET, and DAT were determined. In addition, binding modes of 19 with SERT, NET, and DAT were predicted by docking studies.

中文翻译：

鉴定 1-苯氧基-3-(哌嗪-1-基)丙-2-醇衍生物作为新型三重再摄取抑制剂

新型 1-苯氧基-3-(哌嗪-1-基)丙-2-醇衍生物被设计和合成为潜在的三重再摄取抑制剂，可同时抑制血清素、去甲肾上腺素和多巴胺转运蛋白（分别为 SERT、NET 和 DAT）。通过神经递质转运蛋白摄取测定，评估了 1-苯氧基-3-(哌嗪-1-基)丙-2-醇衍生物的抑制活性。我们发现化合物19对所有三种单胺神经递质转运蛋白表现出最有效的抑制活性，并测定了19对 SERT、NET 和 DAT 的 IC ₅₀值。此外，通过对接研究预测了19与SERT、NET和DAT的结合模式。

更新日期：2023-03-29

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