Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133002, PR China.
Eur J Med Chem. 2012 Feb;48:174-8. doi: 10.1016/j.ejmech.2011.12.011. Epub 2011 Dec 13.
In the present study, a series of 1,3-diaryl pyrazole derivatives bearing rhodanine-3-fatty acid moieties were synthesized and their antimicrobial activities were tested against various Gram-positive and Gram-negative bacteria. 1,3-diaryl-4-formylpyrazoles were synthesized as key intermediates following a Vilsmeier-Haack strategy. Several compounds with an MIC of 2 μg/mL, exhibited stronger antibacterial activity against the methicillin-resistant Staphylococcus aureus (MRSA) than the controls. None of the compounds showed any activity against Gram-negative bacteria.
在本研究中，合成了一系列含有罗丹宁-3-脂肪酸部分的 1,3-二芳基吡唑衍生物，并测试了它们对各种革兰氏阳性菌和革兰氏阴性菌的抗菌活性。1,3-二芳基-4-甲酰基吡唑是通过 Vilsmeier-Haack 策略作为关键中间体合成的。几种 MIC 为 2 μg/mL 的化合物对耐甲氧西林金黄色葡萄球菌（MRSA）的抗菌活性强于对照物。没有一种化合物对革兰氏阴性菌有任何活性。
