3,4-二氢嘧啶-2(1H)- 1类似物:微波辐照合成与抗菌和抗结核研究

IF 0.9 Q4 CHEMISTRY, MULTIDISCIPLINARY Current Microwave Chemistry Pub Date : 2019-10-24 DOI:10.2174/2213335606666190724093305
N. Patel, Sabir S Pathan, Hetal I. Soni
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引用次数: 4

摘要

为了快速、可持续的合成,微波辐照法是可行的。本文研究了用微波辐射法制备含1,2,3,4-四氢嘧啶的恶二唑和吡啶衍生物。本研究旨在通过微波辅助加热快速合成Biginelli产物的恶二唑的氯-乙酰胺和吡啶的氨基氰衍生物。我们的工作重点是在分子框架中引入化学多样性,以合成药理学上有趣的化合物。采用微波辐照Biginelli反应合成了2-((3-氰基-4-(3,4-二氯苯基)- 6-(4-羟基-3-甲氧基苯基)吡啶-2-基)氨基- n-(5-(取代)-(6-甲基-2-氧-1,2,3,4-四氢嘧啶-5-基)-1,3,4-恶二唑-2-基)乙酰胺。通过光谱研究确定了新的结构类似物,并对金黄色葡萄球菌、脓葡萄球菌、大肠杆菌和铜绿假单胞菌进行了体外抑菌活性筛选,对白色念珠菌、黑曲霉和棒曲霉进行了微肉汤稀释法抑菌活性筛选。采用Lowenstein-Jensen培养基对H37Rv(结核分枝杆菌)进行体外抑菌活性测定。与传统方法相比,微波辐照法更有利于1,2,3,4-四氢嘧啶衍生物的合成。部分化合物具有较强的抗菌活性和抗结核活性。微波辐照技术为发现一类新型抗菌和抗结核药物提供了有效途径。1,2,3,4-四氢嘧啶衍生物具有较好的抗菌和抗结核活性。
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3,4-Dihydropyrimidin-2(1H)-One Analogues: Microwave irradiated Synthesis with Antimicrobial and Antituberculosis Study
For rapid and sustainable synthesis, microwave irradiation method is serviceable. This present study deals with the preparation of oxadiazole and pyridine bearing 1,2,3,4- tetrahydro pyrimidine derivatives by microwave irradiation.The present study aims to carry out rapid synthesis of chloro-acetamides of oxadiazoles of Biginelli product and amino cyano derivative of pyridine by microwave-assisted heating. Our efforts are focused on the introduction of chemical diversity in the molecular framework in order to synthesize pharmacologically interesting compounds.Microwave irradiation was used for the synthesis of 2-((3-cyano-4-(3,4-dichloro phenyl)- 6-(4-hydroxy-3-methoxyphenyl) pyridin-2-yl) amino)-N-(5-(substituted) -(6-methyl-2-oxo -1,2,3,4- tetrahydro pyrimidin-5-yl)-1,3,4-oxadiazol-2-yl)acetamide by using Biginelli reaction. New structural analogues were confirmed by spectral studies followed by their screening for in vitro antibacterial activity against Staphylococcus aureus, Staphylococcus Pyogenus, Escherichia coli and Pseudomonas aeruginosa bacterial strains and for antifungal activity against Candida albicans, Aspergillus niger and Aspergillus clavatus by micro-broth dilution method. In vitro antimycobacterial activity determined out against (Mycobacterium tuberculosis) H37Rv strain using Lowenstein-Jensen medium.As compared to the conventional method, microwave irradiation method is advantageous for the synthesis of 1,2,3,4-tetrahydropyrimidin derivatives. Potent antimicrobial activities and antitubercular activity were found for some of the compounds.Microwave irradiation method provided an effective way to discover a novel class of antimicrobial and antituberculosis agents. 1,2,3,4-tetrahydropyrimidin derivatives showed improved antimicrobial and good antituberculosis activity.
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来源期刊
Current Microwave Chemistry
Current Microwave Chemistry CHEMISTRY, MULTIDISCIPLINARY-
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