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Synthesis, anticonvulsant and anti-inflammatory studies of new 1,4-dihydropyridin-4-yl-phenoxyacetohydrazones

机译:1,4-二氢吡啶-4-基苯氧基乙hydr的合成,抗惊厥和抗炎研究

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摘要

The present work involves design and synthesis of new substituted 1,4-dihydropyridin-4-yl-phenoxyacetohydrazones (4a-s, 5a-h), starting from 4-hydroxybenzaldehyde. The final compounds were screened for their in vivo anticonvulsant activity by MES, scPTZ and 6 Hz methods, while their anti-inflammatory screening was performed by Carrageenan induced Paw Edema method. The results indicated that compounds carrying electron donating groups are anticonvulsant active, while most of the tested compounds exhibited significant anti-inflammatory activity. Compounds 4k, l, 4p-s, and 5c showed rapid anti-inflammatory activity within 30 min and appeared as lead compounds. Further, Neurotoxicity study revealed that all the tested compounds are non-toxic up to 300 mg/kg doses. Selected compounds were also subjected to analgesic screening following Tail immersion method and they exhibited good activity.
机译:本工作涉及从4-羟基苯甲醛开始的新型取代的1,4-二氢吡啶-4--4-基-苯氧基乙hydr(4a-s,5a-h)的设计和合成。通过MES,scPTZ和6 Hz方法筛选最终化合物的体内抗惊厥活性,而通过角叉菜胶诱导的爪水肿方法进行抗炎筛选。结果表明,带有供电子基团的化合物具有抗惊厥活性,而大多数受试化合物均具有显着的抗炎活性。化合物4k,1、4p-s和5c在30分钟内显示出快速的抗炎活性,并以先导化合物的形式出现。此外,神经毒性研究表明,所有受试化合物在300 mg / kg剂量以下均无毒。所选化合物还按照尾巴浸没法进行了镇痛筛选,它们显示出良好的活性。

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