吡唑基异恶唑啉类抗菌药物的合成及生物学评价

Rajesh Kumar, Manoj Kumar, C. Sharma, K. R. Aneja, O. Prakash
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引用次数: 0

摘要

在含催化量TFA的甲醇中,在二醋酸碘苯的存在下,吡唑基腈氧化物与各种活性烯烃(丙烯腈、丙烯酸甲酯、醋酸乙烯酯)在室温下以1,3-偶极环加成法合成吡唑基异恶唑啉,探讨其对微生物体外生长引起微生物感染的影响。研究了11种化合物对两种革兰氏阳性菌(金黄色葡萄球菌、枯草芽孢杆菌)和两种革兰氏阴性菌(大肠杆菌和铜绿假单胞菌)的抑菌活性。并对合成的化合物进行了抑菌试验。
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Synthesis and Biological Evaluation of Pyrazolyl Isoxazolines as Antimicrobial Agents
Pyrazolyl isoxazolines were synthesized by 1,3-dipolar cycloaddition of pyrazolyl nitrile oxide with various activated alkene such as acrylonitrile, methyl acrylate and vinyl acetate in the presence of iodobenzene diacetate in methanol containing a catalytic amount of TFA at room temperature with an aim to explore their effect on in vitro growth of microorganism causing microbial infection. Eleven compounds were tested in vitro for their antibacterial activity against two Gram-positive bacteria namely, Staphylococcus aureus , Bacillus subtilis and two Gram-negative bacteria namely, Escherichia coli and Pseudomonas aeruginosa . All the synthesized compounds were also tested for their inhibitory action against two strains of fungus.
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