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合成、抗惊厥和抗炎研究的新 1,4-二氢吡啶-4-基-苯氧基乙酰腙。

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

机构信息

Department of Chemistry, National Institute of Technology Karnataka, Surathkal, Mangalore 575 025, Karnataka, India.

出版信息

Eur J Med Chem. 2013;70:341-9. doi: 10.1016/j.ejmech.2013.10.010. Epub 2013 Oct 12.

Abstract

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.

摘要

本工作涉及新型取代的 1,4-二氢吡啶-4-基-苯氧基乙酰腙(4a-s,5a-h)的设计和合成,从 4-羟基苯甲醛开始。通过 MES、scPTZ 和 6 Hz 方法对最终化合物进行体内抗惊厥活性筛选,通过角叉菜胶诱导的爪肿胀法进行抗炎筛选。结果表明,带有供电子基团的化合物具有抗惊厥活性,而大多数测试化合物表现出显著的抗炎活性。化合物 4k、l、4p-s 和 5c 在 30 分钟内表现出快速的抗炎活性,是潜在的先导化合物。此外,神经毒性研究表明,所有测试化合物在 300mg/kg 剂量下均无毒性。选择的化合物还进行了尾浸法的镇痛筛选,结果表明它们具有良好的活性。

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