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4-氧代和4-硫代-8-溴苯并吡喃衍生物的合成及抗惊厥活性

Synthesis and anticonvulsant activity of 4-oxo and 4-thioxo-8-bromobenzopyran derivatives.

作者信息

Ragab Fatma Abd El-Fattah, Hassan Ghaneya Sayed, Abu Yossef Hanan Al-Sayed, Yahya Tawfeek Ahmed Ali, Abd El-Latif Hekma A

机构信息

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

出版信息

Arzneimittelforschung. 2010;60(4):171-6.

Abstract

Several thiosemicarbazones (7 and 8), 1,3-thiazolidin-4-ones (9, 10, 13, 14) and 2-thioxo-1,3-imidazolidin-4-ones (11) have been prepared starting from 8-bromo-7-hydroxy-5-methoxy-2-methyl-4-oxo-4H-1-benzopyran-6-carbaldehyde (3) and its 4-thio analogue (4). The anticonvulsant activity of all of the synthesized compounds was evaluated against maximal electrical shock (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizures. The neurotoxicity was assessed using the rota-rod test. Some of the tested compounds displayed potent anticonvulsant activity in the scPTZ test.

摘要

已经从8-溴-7-羟基-5-甲氧基-2-甲基-4-氧代-4H-1-苯并吡喃-6-甲醛(3)及其4-硫代类似物(4)出发制备了几种硫代半卡巴腙(7和8)、1,3-噻唑烷-4-酮(9、10、13、14)和2-硫代-1,3-咪唑烷-4-酮(11)。对所有合成化合物针对最大电休克(MES)和皮下注射戊四氮(scPTZ)诱导的癫痫发作的抗惊厥活性进行了评估。使用转棒试验评估神经毒性。一些受试化合物在scPTZ试验中表现出强效抗惊厥活性。

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