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
Reem A. K Al-Harbi
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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。
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.

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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.
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