{"title":"合成含有苯并二恶茂分子的噻唑烷酮和甲基噻唑衍生物并评估其抗菌活性","authors":"Reem A. K Al-Harbi","doi":"10.1080/00397911.2024.2387118","DOIUrl":null,"url":null,"abstract":"<div><p>One of the most serious future challenges to health care professionals is the emergence of multi-drug resistance pathogenic microbes that rapidly develop resistance to currently used antibiotics. So, as a way to overcome the antimicrobial drug-resistance problems, it is urgent need to synthesize several new lead molecules that are expected to have antibacterial and antifungal activities. So, some new thiazolidinone and methylthiazole derivatives incorporating benzodioxole nucleolus were constructed. Two different series of <em>N</em>-substituted thiosemicarbazones carrying a benzodioxole nucleus were synthesized through mutation reaction of the different aromatic and heterocyclic aldehydes with benzodioxolyl thiosemicarbazide. Cycloalkylation reaction of the latter thiosemicarbazones through with both of the ethyl chloroacetate or chloroacetone gave the thiazolidin-4-ones or 4-methylthiazoles, respectively. The antimicrobial activity of the thiazolidin-4-one and 4-methylthiazole derivatives was investigated. All of compounds showed from weak to moderate effects toward all tested bacteria.</p></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":"54 16","pages":"Pages 1366-1375"},"PeriodicalIF":1.8000,"publicationDate":"2024-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis of thiazolidinone and methylthiazole derivatives incorporating benzodioxole moiety and evaluation of their antimicrobial activity\",\"authors\":\"Reem A. K Al-Harbi\",\"doi\":\"10.1080/00397911.2024.2387118\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>One of the most serious future challenges to health care professionals is the emergence of multi-drug resistance pathogenic microbes that rapidly develop resistance to currently used antibiotics. So, as a way to overcome the antimicrobial drug-resistance problems, it is urgent need to synthesize several new lead molecules that are expected to have antibacterial and antifungal activities. So, some new thiazolidinone and methylthiazole derivatives incorporating benzodioxole nucleolus were constructed. Two different series of <em>N</em>-substituted thiosemicarbazones carrying a benzodioxole nucleus were synthesized through mutation reaction of the different aromatic and heterocyclic aldehydes with benzodioxolyl thiosemicarbazide. Cycloalkylation reaction of the latter thiosemicarbazones through with both of the ethyl chloroacetate or chloroacetone gave the thiazolidin-4-ones or 4-methylthiazoles, respectively. The antimicrobial activity of the thiazolidin-4-one and 4-methylthiazole derivatives was investigated. All of compounds showed from weak to moderate effects toward all tested bacteria.</p></div>\",\"PeriodicalId\":22119,\"journal\":{\"name\":\"Synthetic Communications\",\"volume\":\"54 16\",\"pages\":\"Pages 1366-1375\"},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2024-08-17\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Synthetic Communications\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/org/science/article/pii/S003979112400081X\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Synthetic Communications","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/org/science/article/pii/S003979112400081X","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
Synthesis of thiazolidinone and methylthiazole derivatives incorporating benzodioxole moiety and evaluation of their antimicrobial activity
One of the most serious future challenges to health care professionals is the emergence of multi-drug resistance pathogenic microbes that rapidly develop resistance to currently used antibiotics. So, as a way to overcome the antimicrobial drug-resistance problems, it is urgent need to synthesize several new lead molecules that are expected to have antibacterial and antifungal activities. So, some new thiazolidinone and methylthiazole derivatives incorporating benzodioxole nucleolus were constructed. Two different series of N-substituted thiosemicarbazones carrying a benzodioxole nucleus were synthesized through mutation reaction of the different aromatic and heterocyclic aldehydes with benzodioxolyl thiosemicarbazide. Cycloalkylation reaction of the latter thiosemicarbazones through with both of the ethyl chloroacetate or chloroacetone gave the thiazolidin-4-ones or 4-methylthiazoles, respectively. The antimicrobial activity of the thiazolidin-4-one and 4-methylthiazole derivatives was investigated. All of compounds showed from weak to moderate effects toward all tested bacteria.
期刊介绍:
Synthetic Communications presents communications describing new methods, reagents, and other synthetic work pertaining to organic chemistry with sufficient experimental detail to permit reported reactions to be repeated by a chemist reasonably skilled in the art. In addition, the Journal features short, focused review articles discussing topics within its remit of synthetic organic chemistry.