新型 1,3-二苯基-1H-吡唑并[3,4-d]嘧啶化合物的合成及抑菌活性研究。
Synthesis and antibacterial activity of novel 1,3-diphenyl-1H-pyrazoles functionalized with phenylalanine-derived rhodanines.
机构信息
Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Jilin Province, Yanji 133002, PR China.
出版信息
Eur J Med Chem. 2012 Dec;58:112-6. doi: 10.1016/j.ejmech.2012.10.012. Epub 2012 Oct 18.
In the present study, a series of novel 1,3-diphenyl-1H-pyrazoles functionalized with phenylalanine-derived rhodanine derivatives were synthesized and evaluated for their antibacterial activity. Compounds 4, 6, 9, 10, 12 and 15 exhibited stronger activity than the standard drugs, norfloxacin and oxacillin, with MIC values of 1 μg/mL against methicillin-resistant Staphylococcus aureus and quinolone-resistant S. aureus. None of the compounds showed any activity against Gram-negative bacteria.
在本研究中，合成了一系列新型的 1,3-二苯基-1H-吡唑并苯丙氨酸衍生的罗丹宁衍生物，并评估了它们的抗菌活性。化合物 4、6、9、10、12 和 15 对耐甲氧西林金黄色葡萄球菌和耐喹诺酮金黄色葡萄球菌的 MIC 值为 1 μg/mL，活性均强于标准药物诺氟沙星和苯唑西林。这些化合物对革兰氏阴性菌均无活性。
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