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邻苯二甲酰亚胺席夫碱的合成、表征及体内抗惊厥和神经毒性筛选

Synthesis, characterization and in vivo anticonvulsant and neurotoxicity screening of Schiff bases of phthalimide.

作者信息

Bhat Mashooq A, Al-Omar Mohammed A

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Kingdom of Saudi Arabia.

出版信息

Acta Pol Pharm. 2011 May-Jun;68(3):375-80.

PMID:21648191
Abstract

A series of Schiff bases of phthalimide (4a-l) were prepared in satisfactory yields and evaluated for their anticonvulsant and neurotoxicity activities. The structures of all the compounds were in good agreement with elemental analysis and spectral data. All the compounds were active in MES screen and less neurotoxic than phenytoin. Compound 41 having nitro substitution at ortho position of the distal aryl ring emerged as most promising anticonvulsant agent with low neurotoxicity.

摘要

制备了一系列邻苯二甲酰亚胺席夫碱(4a - l),产率令人满意,并对其抗惊厥和神经毒性活性进行了评估。所有化合物的结构与元素分析和光谱数据高度吻合。所有化合物在最大电休克(MES)实验中均有活性,且神经毒性比苯妥英低。在远端芳环邻位具有硝基取代的化合物41成为最有前景的低神经毒性抗惊厥剂。

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