3-(烷基氨基、烷氧基)-1,3,4,5-四氢-2H-苯并[b]氮杂卓-2-酮衍生物的合成及抗惊厥活性。
Synthesis and Anticonvulsant Activity of 3-(alkylamino, alkoxy)-1,3,4,5- Tetrahydro-2H-benzo [b] azepine-2-one Derivatives.
机构信息
Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province, China.
Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules (Yanbian University), Ministry of Education, Yanji, 133002, Jilin Province, China.
出版信息
CNS Neurol Disord Drug Targets. 2018;17(6):448-457. doi: 10.2174/1871527317666180704101332.
BACKGROUND & OBJECTIVE: A series of novel 3-Substituted-1,3,4,5-Tetrahydro-2H-benzo [b] azepine-2-one Derivatives (4, 5, 7, 10, 12, 5a-j, 8a-e) were synthesized from 1,2,3,4-Tetrahydro-1- naphthalenone. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR, MASS spectra and elemental analysis. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. Compound 4 showed the maximum anticonvulsant activity against the maximal electroshock test (ED50=26.4, PI =3.2) and against the subcutaneous pentylenetetrazol test (ED50=40.2, PI =2.1).
CONCLUSION
Possible structure-activity relationship was discussed.
背景与目的
从 1,2,3,4-四氢-1-萘酮合成了一系列新型的 3-取代-1,3,4,5-四氢-2H-苯并[b]氮杂卓-2-酮衍生物（4、5、7、10、12、5a-j、8a-e）。这些化合物的结构通过 IR、1H NMR、13C NMR、MASS 谱和元素分析得到证实。它们的抗惊厥活性通过最大电休克（MES）试验、皮下戊四氮（scPTZ）试验进行评估，其神经毒性通过旋转棒神经毒性试验进行评估。化合物 4 在最大电休克试验（ED50=26.4，PI=3.2）和皮下戊四氮试验（ED50=40.2，PI=2.1）中表现出最大的抗惊厥活性。
结论
讨论了可能的构效关系。
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