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首页> 外文期刊>Journal of the Korean Chemical Society >A Facile Greener Assisted Protocol for the Synthesis of Some New 4-aryl-(5-chloro-3-Methyl-1-phenyl-1H-Pyrazol-4-yl)-4,5-dihydroisoxazol-3-yl) Derivatives and their in vitro Antimicrobial Activity
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A Facile Greener Assisted Protocol for the Synthesis of Some New 4-aryl-(5-chloro-3-Methyl-1-phenyl-1H-Pyrazol-4-yl)-4,5-dihydroisoxazol-3-yl) Derivatives and their in vitro Antimicrobial Activity

机译:一种简便的绿色辅助方案,用于合成一些新的4-芳基-(5-氯-3-甲基-1-苯基-1H-吡唑-4-基)-4,5-二氢异恶唑-3-基)及其衍生物体外抗菌活性

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摘要

An efficient access, single step and environmentally benign synthesis of a new series of pyrazole containing isoxazolines derivatives were prepared by the condensation of chalcones bearing pyrazole moiety with hydroxyl amine hydrochloride in basic condition by using polyethylene glycol-400 (PEG) as a greener reaction solvent. The advantages of the present methodology are mild reaction condition and avoidance of volatile organic solvent. Furthermore, these newly synthesized compounds were screened for their antimicrobial activity against various pathogens like Escherichia coli (MTCC 2939), Salmonella typhi (MTCC 98), Staphylococcus aureus (MTCC 96), Bacillus subtilis (MTCC 441), Aspergillus niger (MTCC 281), Aspergillus flavus (MTCC 2501), Penicillium chrsogenum (MTCC 160) and Fusarium moniliformae (MTCC 156). Especially compound containing the hydroxyl group in C2-position and presence of halo (I, Br and Cl) groups as substituents at C3 and C5 position on the benzene nucleus showed the higher activity. Furthermore, compounds bearing methyl groups in combination with I and Br which enhanced the activity.
机译:聚吡咯部分的查耳酮在碱性条件下,以聚乙二醇-400(PEG)为绿色反应溶剂,通过缩合带有吡唑部分的查耳酮与盐酸羟胺的缩合反应,可高效合成,合成一系列含有异恶唑啉衍生物的新型吡唑。 。本方法的优点是反应条件温和并且避免了挥发性有机溶剂。此外,筛选了这些新合成的化合物对各种病原体(如大肠杆菌(MTCC 2939),伤寒沙门氏菌(MTCC 98),金黄色葡萄球菌(MTCC 96),枯草芽孢杆菌(MTCC 441),黑曲霉(MTCC 281)的抗菌活性。 ,黄曲霉(MTCC 2501),产黄青霉(MTCC 160)和镰刀菌(Fusarium moniliformae)(MTCC 156)。尤其是在苯核的C3和C5位置含C2羟基的羟基和卤素(I,Br和Cl)基团作为取代基的化合物显示出较高的活性。此外,带有甲基和I和Br结合的化合物增强了活性。

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