聊城大学学报（自然科学版）2025，Vol.38Issue(4)：615-624,10.DOI:10.19728/j.issn1672-6634.2024120006
N-(4-(4H-1,2,4-三唑-1-基)苯基)-2-取代苯氧基乙酰胺衍生物的设计、合成及药理活性研究
Design,synthesis and anticonvulsant activity of N-(4-(4H-1,2,4-triazol-1-yl)phenyl)-2-phenoxyacetamide derivatives
摘要
Abstract
In this paper,a series of anticonvulsant derivatives containing triazole structure were designed and synthesized and the structures of the target compounds were confirmed by 1H NMR,13C NMR and HMRS methods.The results of maximal electroshock(MES),subcutaneous pentylenetetrazole(scPTZ)and rotating rod(ROT)assays showed that most of the compounds possessed anticonvulsant activity and low neurotoxicity.Among them,compound 5o showed a PI value of 11.5 and 8.2 in MES and scPTZ ex-periments,respectively,with a higher safety than the positive control carbamazepine of 6.1(MES test)and ethosuximide of 3.5(PTZ test).The test of inhibitory neurotransmitter GABA content in brain tissue further revealed that compound 5o exerted anticonvulsant activity may be associated with increased GABA content in rat brain.The molecular docking results indicated that the potential compound 5o was able to generate significant interaction force with the BZs binding active site amino acid residues of GABAA recep-tor.The results of this study suggest that compound 5o has the potential to serve as a lead compound con-taining a structural fragment of triazole.关键词
三氮唑/合成/抗癫痫/γ-氨基丁酸Key words
triazole/anticonvulsant/synthesis/γ-gaba分类
化学化工引用本文复制引用
李孟娇,胡丽娜,伊世嘉,晋冰冰,雷康,王世本..N-(4-(4H-1,2,4-三唑-1-基)苯基)-2-取代苯氧基乙酰胺衍生物的设计、合成及药理活性研究[J].聊城大学学报（自然科学版）,2025,38(4):615-624,10.基金项目
国家自然科学基金项目(31701827) （31701827）
山东省自然科学基金项目(ZR2022MB064)资助 （ZR2022MB064）
