一些新型查尔酮-磺胺杂化物的设计、合成及生物学评价

Mahammadali M. Khanusiya
{"title":"一些新型查尔酮-磺胺杂化物的设计、合成及生物学评价","authors":"Mahammadali M. Khanusiya","doi":"10.7598/cst2019.1538","DOIUrl":null,"url":null,"abstract":"A series of novel chalcone tethered sulphonamide hybrids 3a-5f were fabricated by condensing appropriate sulphonamide scaffold with methoxy and/or hydroxy substituted chalcones as a multi-target drug for therapeutic treatment. Chalcones were prepared by Claisen-Schmidt condensation of a substituted aldehyde with para aminoacetophenone. The synthesized chalconesulphonamide hybrids were screened by means of their antibacterial activity by NCCLS method. Among all these compounds, 5e and 5c were observed to displaying more potent growth inhibitory activity against bacterial strain and hybrid 5a shows more obvious antifungal activity. FT-IR, NMR and HR-LCMS spectral study assert the structures of synthesized sulphonamide chalcone hybrids.","PeriodicalId":10087,"journal":{"name":"Chemical science transactions","volume":"141 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2019-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"Design, Synthesis and Biological Evaluation of Some Novel Chalcone-Sulfonamide Hybrids\",\"authors\":\"Mahammadali M. Khanusiya\",\"doi\":\"10.7598/cst2019.1538\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A series of novel chalcone tethered sulphonamide hybrids 3a-5f were fabricated by condensing appropriate sulphonamide scaffold with methoxy and/or hydroxy substituted chalcones as a multi-target drug for therapeutic treatment. Chalcones were prepared by Claisen-Schmidt condensation of a substituted aldehyde with para aminoacetophenone. The synthesized chalconesulphonamide hybrids were screened by means of their antibacterial activity by NCCLS method. Among all these compounds, 5e and 5c were observed to displaying more potent growth inhibitory activity against bacterial strain and hybrid 5a shows more obvious antifungal activity. FT-IR, NMR and HR-LCMS spectral study assert the structures of synthesized sulphonamide chalcone hybrids.\",\"PeriodicalId\":10087,\"journal\":{\"name\":\"Chemical science transactions\",\"volume\":\"141 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2019-04-07\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Chemical science transactions\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.7598/cst2019.1538\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemical science transactions","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.7598/cst2019.1538","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 2

摘要

通过适当的磺胺支架与甲氧基和/或羟基取代的查尔酮缩合,制备了一系列新型查尔酮系磺胺杂合体3a-5f,作为多靶点药物进行治疗。以取代醛和对氨基苯乙酮为原料,采用Claisen-Schmidt缩合法制备查尔酮。利用NCCLS法对合成的氯代磺酰胺杂合物进行抑菌活性筛选。其中,5e和5c对菌株的生长抑制活性更强,杂合物5a的抑菌活性更明显。FT-IR、NMR和HR-LCMS对合成的磺胺类查尔酮杂化物的结构进行了表征。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design, Synthesis and Biological Evaluation of Some Novel Chalcone-Sulfonamide Hybrids
A series of novel chalcone tethered sulphonamide hybrids 3a-5f were fabricated by condensing appropriate sulphonamide scaffold with methoxy and/or hydroxy substituted chalcones as a multi-target drug for therapeutic treatment. Chalcones were prepared by Claisen-Schmidt condensation of a substituted aldehyde with para aminoacetophenone. The synthesized chalconesulphonamide hybrids were screened by means of their antibacterial activity by NCCLS method. Among all these compounds, 5e and 5c were observed to displaying more potent growth inhibitory activity against bacterial strain and hybrid 5a shows more obvious antifungal activity. FT-IR, NMR and HR-LCMS spectral study assert the structures of synthesized sulphonamide chalcone hybrids.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
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