Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.

Frecentese F; Fiorino F; Perissutti E; Severino B; Magli E; Esposito A; De Angelis F; Massarelli P; Nencini C; Viti B; Santagada V; Caliendo G

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.

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Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.

机译：新型吲哚芳基哌嗪衍生物作为5-羟色胺能配体的高效微波组合合成。

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An easy and convenient microwave-assisted synthesis of a small library of indolic arylpiperazine derivatives is described. Parallel and mixed pool combinatorial methods are reported and compared. The described reactions are nucleophilic substitutions of several aromatic piperazines in presence of K(2)CO(3). Good yields and short reaction times are the main aspect of these procedures. Binding assays shed additional light on the influence of the LCAPs on the 5-HT(1A), 5-HT(2A) and 5-HT(2C) receptors affinity and allowed to disclose three interesting compounds as 5-HT(2C), mixed 5-HT(2A)/5-HT(2C) and 5-HT(1A)/5-HT(2C) ligands (4i, 4l and 4d, respectively), with potential antiepileptic, anxiolytic or atypical antipsychotic agent therapeutical profiles.

机译：描述了一种简便的微波辅助合成的吲哚基芳基哌嗪衍生物小文库。报告并比较了并行和混合池组合方法。所描述的反应是在K（2）CO（3）存在下几种芳香哌嗪的亲核取代。良好的产率和短的反应时间是这些方法的主要方面。结合试验进一步揭示了LCAP对5-HT（1A），5-HT（2A）和5-HT（2C）受体亲和力的影响，并允许公开三种有趣的化合物，例如5-HT（2C），混合的5-HT（2A）/ 5-HT（2C）和5-HT（1A）/ 5-HT（2C）配体（分别为4i，4l和4d），具有潜在的抗癫痫药，抗焦虑药或非典型抗精神病药的治疗作用。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第2期|共8页
作者
Frecentese F; Fiorino F; Perissutti E; Severino B; Magli E; Esposito A; De Angelis F; Massarelli P; Nencini C; Viti B; Santagada V; Caliendo G;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands. [J] . Frecentese F, Fiorino F, Perissutti E, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第2期

机译：新型吲哚芳基哌嗪衍生物作为5-羟色胺能配体的高效微波组合合成。
2. Benzimidazole derivatives. Part 5: Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT(1A)/5-HT(3) ligands. [J] . Lopez Rodriguez ML, Morcillo MJ, Avila D, Bioorganic and Medicinal Chemistry . 2004,第19期

机译：苯并咪唑衍生物。第5部分：设计和合成新的苯并咪唑-芳基哌嗪衍生物，用作混合的5-HT（1A）/ 5-HT（3）配体。
3. Synthesis and In Vitro Pharmacological Evaluation of Novel 2-Hydroxypropyl-4-arylpiperazine Derivatives as Serotoninergic Ligands [J] . Fiorino Ferdinando, Magli Elisa, Severino Beatrice, Archiv der Pharmazie . 2014,第10期

机译：新型2-羟丙基-4-芳基哌嗪衍生物作为5-羟色胺能配体的合成及体外药理学评价
4. Simple and efficient synthesis of 2,4,5-triarylsubstituted imidazole derivatives via a multicomponent reaction using microwave irradiation [C] . Haitham Dalol Hanoon, Sajid Maksad Radhi, Sawsan Khudhair Abbas International Conference on Applied Science and Technology . 2019

机译：通过使用微波辐射的多组分反应简单有效地合成2,4,5-三芳基二咪唑衍生物
5. I. Structure-based molecular modeling and synthesis of indole derivatives as non-phenolic analogues of mycophenolic acid. II. 3D-QSAR studies using CoMFA on homotropane and tropane derivatives as dopamine transporter and serotonin transporter ligands. [D] . El-Araby, Moustafa El-Sayed. 2001

机译：I.基于结构的分子模型和吲哚衍生物作为霉酚酸的非酚类似物的合成。二。 3D-QSAR研究使用CoMFA对高碘烷和托烷衍生物作为多巴胺转运蛋白和5-羟色胺转运蛋白配体的研究。
6. Microwave-assisted efficient and facile synthesis of tetramic acid derivatives via a one-pot post-Ugi cascade reaction [O] . Yong Li, Zheng Huang, Jia Xu, 2020

机译：通过单池uGI级联反应微波辅助和容易合成四酰胺酸衍生物
7. Rapid Synthesis of Arylpiperazine Derivatives for Imaging 5-HT1AReceptor under Microwave Irradiation [O] . 2005

机译：微波辐射在微波辐射下的成像5-HT1Repeptor的快速合成芳基哌嗪衍生物

Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands.

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