{"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}
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.