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

IF 1.8 3区 化学 Q3 CHEMISTRY, ORGANIC Synthetic Communications Pub Date : 2024-08-17 DOI:10.1080/00397911.2024.2387118
Reem A. K Al-Harbi
{"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}
引用次数: 0

摘要

未来,医疗保健专业人员面临的最严峻挑战之一,就是出现对目前使用的抗生素迅速产生耐药性的多重抗药性病原微生物。因此,作为克服抗菌药耐药性问题的一种方法,迫切需要合成几种有望具有抗菌和抗真菌活性的新先导分子。因此,我们合成了一些含有苯并二噁唑核醇的新噻唑烷酮和甲基噻唑衍生物。通过不同的芳香族和杂环醛与苯并二氧戊环硫代氨基脲的突变反应,合成了两个不同系列的N-取代的带苯并二氧戊环核的硫代氨基脲。这些硫代氨基羰基化合物与氯乙酸乙酯或氯丙酮发生环烷基化反应,分别生成了噻唑烷-4-酮或 4-甲基噻唑。研究了噻唑烷-4-酮和 4-甲基噻唑衍生物的抗菌活性。所有化合物对所有受试细菌都显示出弱到中等程度的作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
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.

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
Synthetic Communications
Synthetic Communications 化学-有机化学
CiteScore
4.40
自引率
4.80%
发文量
156
审稿时长
4.3 months
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.
期刊最新文献
Synthesis and antioxidant activity of 14-Aryl-14H-dibenzo[a,j] xanthene’s and bis(3-hydroxy-5,5′-dimethyl-2-cyclohexene-1-ones) derivatives using silica-tungstosulfonic acid catalyst Novel and efficient process for the synthesis of 1,3,4-oxadiazole containing MBX-4132 as antimicrobial agent in Neisseria gonorrhoeae Novel Schiff bases of quinolin-4(1h)-one: Synthesis, antiproliferative evaluation, apoptosis, cell cycle, autophagy and molecular docking studies in human colon cancer cells Development of an improved and facile synthesis route of the FGFR inhibitor erdafitinib An efficient and practical synthesis of ferroptosis inducer erastin
×
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
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 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 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1