β-Naphthalene Incorporated Thiazole-5-Carboxamides/Thiazole -5- Ketones: Design, Synthesis and Anticonvulsant Screening against Two Seizure Models

M. Arshad, F. Al-Otaibi, G. Mustafa, S. Shousha, A. Alshahrani
{"title":"β-Naphthalene Incorporated Thiazole-5-Carboxamides/Thiazole -5- Ketones: Design, Synthesis and Anticonvulsant Screening against Two Seizure Models","authors":"M. Arshad, F. Al-Otaibi, G. Mustafa, S. Shousha, A. Alshahrani","doi":"10.3844/AJPTSP.2019.27.37","DOIUrl":null,"url":null,"abstract":"A bunch of β-naphthalene incorporated thiazole-5-carboxamides/thiazole -5- ketones (7a-7o& 8a-8e) were prepared by reacting 4-methyl-2-(naphthalen-2-yl)thiazole-5-carbonyl chloride with appropriate amines. Structures of all the compounds were explained by elemental analysis, FT-IR, 1H NMR and mass spectral data. The compounds were evaluated for their anticonvulsant activity employing MES and chemoshock (scPTZ) seizure tests. Neurotoxicity was also assessed. Majority of these compounds exhibited significant activity against both animal models; however, compounds 7e, 7j, 7n and 8c displayed promising activity and could be considered as leads for further investigations.","PeriodicalId":7769,"journal":{"name":"American Journal of Pharmacology and Toxicology","volume":"24 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"American Journal of Pharmacology and Toxicology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3844/AJPTSP.2019.27.37","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

Abstract

A bunch of β-naphthalene incorporated thiazole-5-carboxamides/thiazole -5- ketones (7a-7o& 8a-8e) were prepared by reacting 4-methyl-2-(naphthalen-2-yl)thiazole-5-carbonyl chloride with appropriate amines. Structures of all the compounds were explained by elemental analysis, FT-IR, 1H NMR and mass spectral data. The compounds were evaluated for their anticonvulsant activity employing MES and chemoshock (scPTZ) seizure tests. Neurotoxicity was also assessed. Majority of these compounds exhibited significant activity against both animal models; however, compounds 7e, 7j, 7n and 8c displayed promising activity and could be considered as leads for further investigations.
β-萘结合噻唑-5-羧胺类/噻唑-5-酮类:设计、合成及抗惊厥药物筛选
利用4-甲基-2-(萘-2-基)噻唑-5-羰基氯与适当的胺反应,制备了一组β-萘掺入噻唑-5-羧酰胺/噻唑-5-酮(7a- 70和8a-8e)。所有化合物的结构均通过元素分析、FT-IR、1H NMR和质谱数据进行了解释。采用MES和化学休克(scPTZ)发作试验评估化合物的抗惊厥活性。还评估了神经毒性。这些化合物大多数对两种动物模型都有显著的活性;化合物7e, 7j, 7n和8c显示出良好的活性,可以作为进一步研究的线索。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信