Synthesis, physicochemical characterization and analgesic evaluation of some new thieno [2,3-D] Pyrimidin 4(3H) one derivatives

Dinesh P Kawade, D. Chaple, P. Khedekar
{"title":"Synthesis, physicochemical characterization and analgesic evaluation of some new thieno [2,3-D] Pyrimidin 4(3H) one derivatives","authors":"Dinesh P Kawade, D. Chaple, P. Khedekar","doi":"10.18231/j.ijpca.2020.005","DOIUrl":null,"url":null,"abstract":"A POCl3 catalyzed, efficient, one-step and solvent-free synthesis of novel thieno [2,3-d] pyrimidin-4(3H)-one derivatives from 2-amino-4,5-substitutedthiophene-3-carbonitrile has been developed using various aliphatic acid under both conventional heating and microwave irradiation techniques. The formation of compounds was confirmed via elemental analysis and spectroscopic techniques like FTIR, 1HNMR and mass spectroscopy. All synthesized compounds have been screened for their analgesic activity by using Eddy´s hot plate method. The synthesized compounds 2d, 2k and 2h showed good analgesic activity and compounds 2a, 2b, 2g and 2i showed moderate whereas remaining compounds possessed less analgesic activity compared with standard, Tramadol. \n\nKeywords: POCl3, Thieno[2,3-d]pyrimidin-4 (3H)-one, Analgesic activity, Eddy´s hot plate.","PeriodicalId":14317,"journal":{"name":"International Journal of Pharmaceutical Chemistry","volume":"28 1","pages":"32-38"},"PeriodicalIF":0.0000,"publicationDate":"2020-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Pharmaceutical Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.18231/j.ijpca.2020.005","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 1

Abstract

A POCl3 catalyzed, efficient, one-step and solvent-free synthesis of novel thieno [2,3-d] pyrimidin-4(3H)-one derivatives from 2-amino-4,5-substitutedthiophene-3-carbonitrile has been developed using various aliphatic acid under both conventional heating and microwave irradiation techniques. The formation of compounds was confirmed via elemental analysis and spectroscopic techniques like FTIR, 1HNMR and mass spectroscopy. All synthesized compounds have been screened for their analgesic activity by using Eddy´s hot plate method. The synthesized compounds 2d, 2k and 2h showed good analgesic activity and compounds 2a, 2b, 2g and 2i showed moderate whereas remaining compounds possessed less analgesic activity compared with standard, Tramadol. Keywords: POCl3, Thieno[2,3-d]pyrimidin-4 (3H)-one, Analgesic activity, Eddy´s hot plate.
新型噻吩[2,3- d]嘧啶4(3H) 1衍生物的合成、理化性质及镇痛评价
以不同的脂肪酸为原料,在常规加热和微波辐照下,催化POCl3高效一步无溶剂合成了2-氨基-4,5-取代噻吩-3-碳腈的新型噻吩[2,3-d]嘧啶-4(3H)- 1衍生物。通过元素分析和FTIR、1HNMR和质谱等光谱技术证实了化合物的形成。所有合成的化合物都用Eddy ' s热板法进行了镇痛活性筛选。合成的化合物2d、2k和2h具有良好的镇痛活性,化合物2a、2b、2g和2i具有中等的镇痛活性,其余化合物与标准曲马多相比具有较低的镇痛活性。关键词:POCl3, Thieno[2,3-d]嘧啶-4 (3H)- 1,镇痛活性,涡流热板
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:481959085
Book学术官方微信