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新型双环吡啶基杂合体与 1,2,3-三唑单元相连:通过点击反应合成及神经毒性活性评价和分子对接。

New Bicyclic Pyridine-Based Hybrids Linked to the 1,2,3-Triazole Unit: Synthesis via Click Reaction and Evaluation of Neurotropic Activity and Molecular Docking.

机构信息

Scientific Technological Center of Organic and Pharmaceutical Chemistry of National Academy of Science of Republic of Armenia, Institute of Fine Organic Chemistry of A.L.Mnjoyan, Ave. Azatutyan 26, Yerevan 0014, Armenia.

Dipartimento di Chimica G. Ciamician, Alma Mater Studiorum-Università di Bologna, Via F. Selmi 2, 40126 Bologna, Italy.

出版信息

Molecules. 2023 Jan 17;28(3):921. doi: 10.3390/molecules28030921.

Abstract

The synthesis of new original bicyclic pyridine-based hybrids linked to the 1,2,3-triazole unit was described via a click reaction. The anticonvulsant activity and some psychotropic properties of the new compounds were evaluated. The biological assays demonstrated that some of the studied compounds showed high anticonvulsant and psychotropic properties. The five most active compounds (, , , , and ) contain a pyrano [3,4-]pyridine cycle with a methyl group in the pyridine ring in their structures. Furthermore, molecular docking studies were performed, and their results are in agreement with experimental data.

摘要

通过点击反应,描述了新的原始双环吡啶基杂环与 1,2,3-三唑单元的连接的合成。评估了新化合物的抗惊厥活性和一些精神药物特性。生物测定表明,一些研究的化合物表现出高的抗惊厥和精神药物特性。五个最活跃的化合物(,,,,和)在其结构中含有吡啶环中的甲基的吡喃并[3,4-]吡啶环。此外,还进行了分子对接研究,其结果与实验数据一致。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ed8e/9920413/d32217818368/molecules-28-00921-sch001.jpg

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