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某些新型(2E)-2-[1-芳基-3-(1H-咪唑-1-基)亚丙基]-N-(芳基/H)肼甲酰胺的抗惊厥潜力

Anticonvulsant potential of certain new (2E)-2-[1-Aryl-3-(1H-imidazol-1-yl)propylidene]-N-(aryl/H)hydrazinecarboxamides.

作者信息

Attia Mohamed I, Aboul-Enein Mohamed N, El-Azzouny Aida A, Maklad Yousreya A, Ghabbour Hazem A

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia ; Pharmaceutical and Drug Industries Research Division, Medicinal and Pharmaceutical Chemistry Department (Medicinal Chemistry Group), National Research Centre, Dokki, Giza 12622, Egypt.

Pharmaceutical and Drug Industries Research Division, Medicinal and Pharmaceutical Chemistry Department (Medicinal Chemistry Group), National Research Centre, Dokki, Giza 12622, Egypt.

出版信息

ScientificWorldJournal. 2014 Jan 12;2014:357403. doi: 10.1155/2014/357403. eCollection 2014.

DOI:10.1155/2014/357403
PMID:24523636
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3913509/
Abstract

Anticonvulsant potential and neurotoxicity of certain new imidazole-containing arylsemicarbazones 6a-p are reported. The test compounds 6a-p exhibited anticonvulsant activity mainly in the scPTZ screen. Compound 6p emerged as the most active surrogate displaying 100% protection at a dose level of 636 μ mol/kg in the scPTZ screen without any neurotoxicity. The assigned (E)-configuration of the title compounds 6a-p was confirmed via single crystal X-ray structure of compound 6g.

摘要

报道了某些含咪唑的新型芳基氨基脲6a-p的抗惊厥潜力和神经毒性。测试化合物6a-p主要在皮下注射戊四氮(scPTZ)筛选中表现出抗惊厥活性。化合物6p在scPTZ筛选中在636 μmol/kg的剂量水平下显示出100%的保护作用且无任何神经毒性,成为最具活性的替代物。通过化合物6g的单晶X射线结构确定了标题化合物6a-p的指定(E)-构型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/7e942a84cc54/TSWJ2014-357403.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/632cfa2d7c5c/TSWJ2014-357403.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/66364e99bf6e/TSWJ2014-357403.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/99df4978a1e4/TSWJ2014-357403.sch.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/7e942a84cc54/TSWJ2014-357403.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/632cfa2d7c5c/TSWJ2014-357403.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/66364e99bf6e/TSWJ2014-357403.sch.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/99df4978a1e4/TSWJ2014-357403.sch.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51dc/3913509/7e942a84cc54/TSWJ2014-357403.002.jpg

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