首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta(2)-1,2,4-thiadiazoline.
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Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta(2)-1,2,4-thiadiazoline.

机译:某些新型3-芳基氨基/氨基-4-芳基-5-亚氨基-Delta(2)-1,2,4-噻二唑啉的合成及抗惊厥活性。

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摘要

A series of 3-aryl amino/amino-4-aryl-5-imino-Delta(2)-1,2,4-thiadiazoline have been synthesized using an appropriate synthetic route and characterized by elemental analyses and spectral data. The anticonvulsant activity of all the synthesized compounds was evaluated against maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (ScPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. All the test compounds were administered at doses of 30, 100, and 300mg/kg body weight and the anticonvulsant activity was noted at 0.5 and 4h time intervals after the drug administration. Some of the compounds were evaluated for the Phenobarbitone induced hypnosis potentiation test. Among the compounds tested, all except 2h showed protection from MES seizures, whereas only 3b was found to be active in the ScPTZ test.
机译:使用适当的合成路线合成了一系列3-芳基氨基/氨基-4-芳基-5-亚氨基-δ(2)-1,2,4-噻二唑啉,并通过元素分析和光谱数据进行了表征。评估了所有合成化合物对小鼠最大电击诱发癫痫发作(MES)和皮下戊四氮(ScPTZ)诱发癫痫发作模型的抗惊厥活性。使用转子法评估神经毒性。所有测试化合物均以30、100和300mg / kg体重的剂量给药,并在给药后0.5和4h的时间间隔观察到抗惊厥活性。对某些化合物进行了苯巴比妥诱导的催眠增强试验的评价。在测试的化合物中,除2h以外的所有化合物均显示出对MES发作的保护,而在ScPTZ测试中仅发现3b具有活性。

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