Khaligh Pooneh, Salehi Peyman, Bararjanian Morteza, Aliahmadi Atousa, Khavasi Hamid Reza, Nejad-Ebrahimi Samad
Department of Phytochemistry, Medicinal Plants and Drugs Research Institute, Shahid Beheshti University.
Chem Pharm Bull (Tokyo). 2016;64(11):1589-1596. doi: 10.1248/cpb.c16-00463.
Menthyl 1,4-disubstituted 1,2,3-triazole derivatives of hydroxybenzaldehydes, phenols and bile acids were synthesized via click chemistry. The novel synthesized compounds were evaluated for their in vitro antibacterial activity against Enterococcus faecium, and Staphylococcus aureus as Gram-positive bacteria. Some derivatives illustrated strong inhibitory effect against E. faecium with the minimum inhibitory concentration (MIC) values ranged from 1-3 µM, where cefixime as a positive control revealed MIC value of 35 µM. The structures of the synthesized compounds were confirmed by different spectroscopic techniques including H-NMR, C-NMR, high resolution (HR)-MS, IR and X-ray crystallographic analysis.
通过点击化学合成了羟基苯甲醛、苯酚和胆汁酸的薄荷基1,4-二取代1,2,3-三唑衍生物。对新合成的化合物进行了体外抗粪肠球菌和金黄色葡萄球菌这两种革兰氏阳性菌的抗菌活性评估。一些衍生物对粪肠球菌表现出强烈的抑制作用，最低抑菌浓度（MIC）值在1-3 μM范围内，而作为阳性对照的头孢克肟的MIC值为35 μM。通过包括H-NMR、C-NMR、高分辨率（HR）-MS、IR和X射线晶体学分析在内的不同光谱技术对合成化合物的结构进行了确证。
