| 陈士龙,郭东福,喻圣旺,何世辉,赵文豪,邓先清.1-(3-苯氧基丙基)-1H-1,2,4-三氮唑衍生物的合成及其抗惊厥活性[J].井冈山大学自然版,2019,40(1):88-93,98 |
| 1-(3-苯氧基丙基)-1H-1,2,4-三氮唑衍生物的合成及其抗惊厥活性 |
| SYNTHESIS OF 1-(3-PHENOXYPROPYL)-1H-1,2,4-TRIAZOLE DERIVATIVES AND THEIR ANTICONVULSANT ACTIVITIES |
| 投稿时间：2018-10-01 修订日期：2018-11-21 |
| DOI：10.3969/j.issn.1674-8085.2019.01.018 |
| 中文关键词: 三氮唑 抗癫痫 最大电休克发作模型 戊四唑 |
| 英文关键词: triazole anticonvulsant maximal electroshock shock sc-PTZ |
| 基金项目:国家自然科学基金项目（21562028）；井冈山大学第七批校级大学生创新创业训练计划项目 |
| 作者 | 单位 | | 陈士龙 | 井冈山大学医学部, 江西, 吉安 343009 | | 郭东福 | 井冈山大学医学部, 江西, 吉安 343009 | | 喻圣旺 | 井冈山大学医学部, 江西, 吉安 343009 | | 何世辉 | 井冈山大学医学部, 江西, 吉安 343009 | | 赵文豪 | 井冈山大学医学部, 江西, 吉安 343009 | | 邓先清 | 井冈山大学医学部, 江西, 吉安 343009 |
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| 中文摘要: |
| 目的 合成一系列1-(3-苯氧基丙基)-1H-1,2,4-三氮唑衍生物，对其体内抗惊厥活性进行研究。方法 以取代酚为起始原料，先后与1-溴-3-氯丙烷及1,2,4-三氮唑进行烷基化反应，得到目标化合物2a-2m。化合物2a-2m通过核磁共振氢谱、碳谱和质谱进行结构确证；采用最大电休克发作模型和皮下戊四唑模型评价目标化合物的抗惊厥活性，旋转棒法评价目标化合物的神经毒性。结果 合成了一系列单烷基取代的三唑类衍生物，这些化合物对MES模型和Sc-PTZ模型均有效，大部分在100 mg/kg剂量下表现出抗惊厥活性，使得该类化合物具有广谱的抗癫痫潜能。结论 新合成的(3-苯氧基丙基)-1H-1,2,4-三氮唑衍生物具有较好的抗惊厥活性，使得该类化合物具有广谱的抗癫痫潜能。本研究进一步丰富了三唑类化合物的抗癫痫构效关系，同时为研究大发作和失神发作类癫痫的治疗药物提供了一定的基础。 |
| 英文摘要: |
| Objective: To synthesize a series of 1-(3-phenoxypropyl)-1H-1,2,4-triazole derivatives and investigate their anticonvulsant effects. Methods: Various phenols were used as the starting material, which reacted with 1-bromo-3-chloropropane and 1,2,4-triazole in sequential order to provide the target compounds 2a-2m. The structures of these compounds were confirmed by 1H-NMR, 13C-NMR, and MS spectrum. Their anticonvulsant activities were evaluated using maximal electroshock shock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure models in mice. The neurotoxicity was evaluated with rotating rod test. Results: A series of alkyl substituted triazoles were synthesized, and their anticonvulsant activities were confirmed by the both models. Conclusion: The alkyl substituted triazoles reported in this work exhibited broad-spectrum anticonvulsant activity. This found enriches the antiepileptic structure-activity relationships of triazole compounds, and provides the reference, to some extent, to the research and development of new drugs of the grand and apathetic seizures. |
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