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N-氨基琥珀酰亚胺的合成与抗惊厥活性评价

Synthesis and anticonvulsant evaluation of N-aminosuccinimides.

作者信息

Kornet M J

出版信息

J Pharm Sci. 1984 Mar;73(3):405-6. doi: 10.1002/jps.2600730332.

Abstract

Twelve new N-aminosuccinimides were synthesized by the condensation of hydrazines with succinic anhydrides in glacial acetic acid. The compounds were evaluated in the maximal electroshock seizure and subcutaneous pentylenetetrazol seizure threshold tests for anticonvulsant activity and in the rotorod test for neurotoxicity in mice. The lowest dose at which several of the compounds exhibited anticonvulsant activity was 300 mg/kg.

摘要

通过肼与琥珀酸酐在冰醋酸中缩合反应合成了12种新型N-氨基琥珀酰亚胺。在最大电休克惊厥和皮下注射戊四氮惊厥阈值试验中评估这些化合物的抗惊厥活性,并在小鼠转棒试验中评估其神经毒性。几种化合物表现出抗惊厥活性的最低剂量为300mg/kg。

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