{"title":"Synthesis of functionalized sulfonamides as antitubercular agents","authors":"M. Hearn, Catherine D. Pugh, M. Cynamon","doi":"10.1080/10426507.2023.2196079","DOIUrl":null,"url":null,"abstract":"Abstract Using up-to-date methods for synthesis and analysis, 51 sulfonamides were prepared for use as tools in antitubercular drug discovery. The synthetic efforts were centered on varying substituents at three key structural units implicated in antimicrobial activity, namely the sulfonyl group, nitrogen N1 and nitrogen N4. Procedures were specific to the sites of functionalization. Preliminary biological assessments are included here on selected compounds. The results suggest that the compounds may be useful in the exploration of the likely interactions of sulfa drugs with enzymes found in tuberculosis (dihydropteroate synthase) or its human host (N-acetyltransferase), interactions that result in drug activity or drug de-activation, respectively. GRAPHICAL ABSTRACT","PeriodicalId":20043,"journal":{"name":"Phosphorus Sulfur and Silicon and The Related Elements","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2023-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Phosphorus Sulfur and Silicon and The Related Elements","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/10426507.2023.2196079","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
Abstract Using up-to-date methods for synthesis and analysis, 51 sulfonamides were prepared for use as tools in antitubercular drug discovery. The synthetic efforts were centered on varying substituents at three key structural units implicated in antimicrobial activity, namely the sulfonyl group, nitrogen N1 and nitrogen N4. Procedures were specific to the sites of functionalization. Preliminary biological assessments are included here on selected compounds. The results suggest that the compounds may be useful in the exploration of the likely interactions of sulfa drugs with enzymes found in tuberculosis (dihydropteroate synthase) or its human host (N-acetyltransferase), interactions that result in drug activity or drug de-activation, respectively. GRAPHICAL ABSTRACT