一些新型异恶唑衍生物的合成、表征及抗菌活性研究

Q2 Chemistry Current Chemistry Letters Pub Date : 2022-01-01 DOI:10.5267/j.ccl.2022.4.004
M. F. Dhaduk, H. Joshi
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引用次数: 1

摘要

以冰醋酸为原料,在回流温度下,1-芳基-3-[5-(4-硝基苯基)-2-呋喃基]-2 -烯-1-酮(4a-j)与盐酸羟胺在乙酸钠存在下进行环缩合反应合成了一系列异恶唑衍生物3-芳基-5-[5-(4-硝基苯基)-2-呋喃基]-2,3-二氢异恶唑(5a-j)。以前,化合物(4a-j)是由5-(4-硝基苯基)呋喃-2-乙醛(3)与各种芳香酮在碱催化下缩合而成。通过元素分析、红外、核磁共振等手段对合成的各种异恶唑的结构进行了表征,并用质谱对其结构进行了进一步的表征。所有产品在浓度为40µg/ml时对革兰氏阳性和革兰氏阴性菌株的抑菌活性以及对黑曲霉的抑菌活性进行了体外生物实验筛选。结果表明,化合物5a、5c、5e、5f和5i与标准对照品相比,具有较好的抗菌和抗真菌活性。
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Synthesis, characterization and antimicrobial activity of some new isoxazole derivatives
A series of isoxazole derivatives, 3-aryl-5-[5-(4-nitrophenyl)-2-furyl]-2,3-dihydroisoxazoles (5a-j) were synthesized by cyclocondensation reaction between 1-aryl-3-[5-(4-nitrophenyl)-2-furyl]prop-2-en-1-ones (4a-j) and hydroxylamine hydrochloride in presence of sodium acetate in glacial acetic acid at reflux temperature. Formerly, compounds (4a-j) were synthesized by the condensation of 5-(4-nitrophenyl) furan-2-carbaldehyde (3) with various aromatic ketones by using alkali as catalyst. The structures of the synthesized various isoxazole have been characterized by using elemental analysis, Infrared,1H-NMR spectroscopy and further supported by Mass spectroscopy. All the products have been screened for their in-vitro biological assay like antibacterial activity towards Gram-positive and Gram-negative bacterial strains and antifungal activity towards Aspergillus niger at a concentration of 40 µg/ml. It was exposed that the compounds 5a, 5c, 5e, 5f, and 5i showed inspiring antibacterial and antifungal activity compared to the used reference standard.
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来源期刊
Current Chemistry Letters
Current Chemistry Letters Chemistry-Chemistry (all)
CiteScore
4.90
自引率
0.00%
发文量
27
审稿时长
20 weeks
期刊介绍: The "Current Chemistry Letters" is a peer-reviewed international journal which aims to publish all the current and outstanding research articles, reviews and letters in chemistry including analytical chemistry, green chemistry, inorganic chemistry, organic chemistry, physical chemistry, etc. This journal is dedicated to serve all academic and industrial researchers and scientists who are expert in all major advances in chemistry research. The journal aims to provide the most complete and reliable source of information on current developments in these fields. The emphasis will be on publishing quality articles rapidly and openly available to researchers worldwide. Please note readers are free to read, download, copy, distribute, print, search, or link to the full texts of articles published on this journal. Current Chemistry Letters is an open access journal, which provides instant access to the full text of research papers without any need for a subscription to the journal where the papers are published. Therefore, anyone has the opportunity to copy, use, redistribute, transmit/display the work publicly and to distribute derivative works, in any sort of digital form for any responsible purpose, subject to appropriate attribution of authorship. Authors who publish their articles may also maintain the copyright of their articles.
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