首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Design and synthesis of antimicrobial, anticoagulant, and anticholinesterase hybrid molecules from 4-methylumbelliferone
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Design and synthesis of antimicrobial, anticoagulant, and anticholinesterase hybrid molecules from 4-methylumbelliferone

机译:从4-甲基伞形酮设计和合成抗微生物,抗凝血和抗胆碱酯酶杂合分子

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Abstract We designed and synthesized new series of diverse triazoles, isoxazoles, isoxazolines, and aziridines linked 4-methylumbelliferone 1 using intermolecular 1,3-dipolar cycloaddition reactions. Structures of these compounds were established on the basis of 1H NMR, 13C NMR, and ESI-HRMS. All prepared compounds were evaluated for their antimicrobial, anticoagulant, and anticholinesterase activities. Interestingly, among the tested molecules, some of the analogs displayed better activities than the parent 4-methylumbelliferone 1 such as 6a and 6d for their antifungal properties. Moreover, compounds 4 , 5 , 6 , and 7 showed the importance of the added fragments to 4-methylumbelliferone 1 via the linker methylene to have good activity.
机译:摘要我们设计并合成了一系列新的三唑,异恶唑,异恶唑啉和氮丙啶,它们通过分子间的1,3-偶极环加成反应连接了4-甲基伞形酮1。这些化合物的结构基于 1 H NMR, 13 C NMR和ESI-HRMS建立。评价所有制备的化合物的抗微生物,抗凝血和抗胆碱酯酶活性。有趣的是,在测试的分子中,一些类似物的抗真菌特性显示出比母体4-甲基伞形酮1更好的活性,例如6a和6d。此外,化合物4、5、6和7显示出通过连接基亚甲基向4-甲基伞形酮1添加的片段具有良好活性的重要性。

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