新型2,5 -二取代四唑衍生物强效生物制剂的合成

Q2 Chemistry Current Chemistry Letters Pub Date : 2023-01-01 DOI:10.5267/j.ccl.2022.11.006
G. V. Megha, Y. Bodke, H. Shanavaz
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引用次数: 0

摘要

本文讨论了以碳酸钾为原料,由1-((2'-(2-(2-(取代苯基))-2-氧乙基)- 2h -四唑-5-基)-[1,1'-联苯]-4-基)甲基)胡椒啶-4-羧酸与苯酰溴反应合成一系列1-((2'-(2-(2-(2-(取代苯基))-2-氧乙基)- 2h -四唑-5-基)-[1,1'-联苯]-4-基)甲基)胡椒啶-4-羧酸衍生物。利用FT-IR, 1H-NMR, 13C-NMR和Mass等不同的光谱技术对合成衍生物的结构进行了表征。对合成的化合物进行抑菌和抗结核活性筛选,所有化合物对选定的病原菌均有较好的抑菌活性。此外,还对靶向酶DNA旋切酶和3-氧酰基- acp还原酶与adme进行了分子对接研究,进行了毒理学研究。
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Synthesis of novel 2, 5-disubstituted tetrazole derivatives as potent biological agents
In the present work, we have discussed the synthesis of a series of 1-((2'-(2-(2-(substitutedphenyl))-2-oxoethyl)-2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)piperidine-4-carboxylic acid derivatives by the reaction of 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)piperidine-4-carboxylic acid with phenacyl bromides using potassium carbonate. The structures of synthesized derivatives have been characterized using different spectroscopic techniques like FT-IR, 1H-NMR, 13C-NMR, and Mass. Synthesized compounds were screened for their antibacterial and anti-TB activities all the compounds have found better activity against selected pathogenic strains. In addition, in silco molecular docking studies were carried out on targeted enzymes DNA gyrase and 3-oxoacyl-ACP reductase with ADME-toxicology studies.
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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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