Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives

doi:10.6023/cjoc201703019

Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (9): 2322-2327.DOI: 10.6023/cjoc201703019 Previous Articles Next Articles

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酞嗪并三唑或四唑类衍生物的合成及其抗惊厥活性研究

张海明, 张洪健, 田玉顺, 全哲山

延边大学药学院延吉 133002

收稿日期:2017-03-02 修回日期:2017-03-30 发布日期:2017-05-17
通讯作者: 田玉顺 E-mail:ld-l@163.com
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

Zhang Haiming, Zhang Hongjian, Tian Yushun, Quan Zheshan

College of Pharmacy, Yanbian University, Yanji 133002

Received:2017-03-02 Revised:2017-03-30 Published:2017-05-17
Contact: 10.6023/cjoc201703019 E-mail:ld-l@163.com
Supported by:
Project supported by the National Natural Science Foundation of China (No. 21272005).

1. Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives.PDF(4290KB)

Abstract

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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Zhang Haiming, Zhang Hongjian, Tian Yushun, Quan Zheshan. Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives[J]. Chin. J. Org. Chem., 2017, 37(9): 2322-2327.

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酞嗪并三唑或四唑类衍生物的合成及其抗惊厥活性研究

Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives

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