酞嗪并三唑或四唑类衍生物的合成及其抗惊厥活性研究
收稿日期: 2017-03-02
修回日期: 2017-03-30
网络出版日期: 2017-05-17
基金资助
国家自然科学基金（No.21272005）资助项目.
Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives
Received date: 2017-03-02
Revised date: 2017-03-30
Online published: 2017-05-17
Supported by
Project supported by the National Natural Science Foundation of China (No. 21272005).
张海明 , 张洪健 , 田玉顺 , 全哲山 . 酞嗪并三唑或四唑类衍生物的合成及其抗惊厥活性研究[J]. 有机化学, 2017 , 37(9) : 2322 -2327 . DOI: 10.6023/cjoc201703019
Four series of derivatives, 6-substituted-1,2,4-triazolo[3,4-a] phthalazine derivatives and 6-substituted tetrazolo[5,1-a]phthalazine derivatives have been synthesized. The structures of compounds are confirmed by 1H NMR, 13C NMR, IR and HRMS. The anticonvulsant effects of the compounds are evaluated with maximal electroshock test by intraperitoneally injected in mice. The experimental results show that N-(4-bromophenyl)tetrazolo[5,1-a]phthalazin-6-amine (7a) was the most potent compound, with a median effective dose of 5.89 mg·kg-1. Its anticonvulsant effect is better than the reference drug, carbamazepine.
Key words： phthalazine; triazolo; tetrazolo; synthesis; anticonvulsant; the maximal electroshock
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