Anticonvulsant Activities of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-ones and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones

Asif Mohammad; Singh Anita

首页> 外文期刊>Open Pharmaceutical Sciences Journal >Anticonvulsant Activities of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-ones and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones

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Anticonvulsant Activities of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-ones and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones

机译：4-亚苄基-6-（4-甲基-苯基）-4,5-二氢哒嗪-（2H）-和4-亚苄基-6-（4-氯-苯基）-4,5-二氢哒嗪-（（ 2H）-个

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Background:Two series of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-one compounds (3a-e) and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones (3f-j) were synthesized and evaluated as anticonvulsant agents.Methods:Synthesized compounds (3a-3j) were tested against maximum electro shock (MES) and Isoniazid (INH) induced convulsion methods for anticonvulsant activities and neurotoxicity.Results:In MES induced convulsions, result found that the compounds 3e and 3j exhibited highest anticonvulsant activities. In INH induced convulsions, result was indicated that all the compounds exhibited good anticonvulsant activities., whereas compounds 3d and 3j showed maximum activity. Methyl derivatives were more active than chloro derivatives. Phenytoin sodium (25mg/kg) and sodium vaproate (50mg/kg) were used as reference drugs. All these synthesized pyridazinone compounds (3a-j) did not exhibit any neurotoxicity up to 100 mg/kg dose levels.Conclusion:All compounds showed good anticonvulsant activities against both MES and INH induced convulsion models. Many such explorations are anticipated in the near future.

机译：背景：两个系列的4-亚苄基-6-（4-甲基-苯基）-4,5-二氢哒嗪-（2H）-一化合物（3a-e）和4-亚苄基-6-（4-氯-苯基）合成了-4,5-二氢哒嗪-（2H）-一（3f-j），并作为抗惊厥药进行了评价。方法：对合成的化合物（3a-3j）进行了最大电击（MES）和异烟肼（INH）诱发惊厥试验。结果：在MES引起的惊厥中，结果发现化合物3e和3j表现出最高的抗惊厥活性。在INH引起的惊厥中，结果表明所有化合物均表现出良好的抗惊厥活性，而化合物3d和3j则表现出最大活性。甲基衍生物比氯衍生物更具活性。苯妥英钠（25mg / kg）和丙戊酸钠（50mg / kg）用作参考药物。所有这些合成的哒嗪酮化合物（3a-j）直至100 mg / kg剂量水平都没有表现出任何神经毒性。结论：所有化合物均对MES和INH诱发的惊厥模型均表现出良好的抗惊厥活性。预计在不久的将来会有许多这样的探索。

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《Open Pharmaceutical Sciences Journal》 |2016年第1期|共12页
作者
Asif Mohammad; Singh Anita;
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中图分类药学;
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AnticonvulsantIsoniazidMaximum electro shockPyridazinonesSynthesis;

机译：抗惊厥药异烟肼最大电击吡啶并酮合成;

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Anticonvulsant Activities of 4-benzylidene-6-(4-methyl-phenyl)-4,5-dihydropyridazin-(2H)-ones and 4-benzylidene-6-(4-chloro-phenyl)-4,5-dihydropyridazin-(2H)-ones

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