Liu Ming-Liang, Pan Xue-Ying, Yang Teng, Zhang Wen-Ming, Wang Tian-Qi, Wang He-Yun, Lin Hai-Xia, Yang Cai-Guang, Cui Yong-Mei
Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University, Shanghai 200444, China.
Nano Science and Technology Institute, University of Science and Technology of China, Suzhou 215123, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Bioorg Med Chem Lett. 2016 Nov 15;26(22):5492-5496. doi: 10.1016/j.bmcl.2016.10.018. Epub 2016 Oct 12.
A series of 12-oxime and O-oxime ether derivatives of dehydroabietic acid were synthesized and investigated for the antibacterial activity against Staphylococcus aureus Newman strain and five multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). The aromatic oximate derivative 11a showed the highest activity with MIC of 0.39-0.78μg/mL against S. aureus Newman. Of note, compounds 10b, 11 and 14 showed the most potent antibacterial activity against five multidrug-resistant S. aureus with MIC values of 1.25-3.13μg/mL. These results offered useful information for further strategic optimization in search of the antibacterial candidates against infection of multidrug-resistant Gram-positive bacteria.
合成了一系列脱氢枞酸的12-肟和O-肟醚衍生物，并研究了它们对金黄色葡萄球菌纽曼菌株和五种耐多药菌株（NRS-1、NRS-70、NRS-100、NRS-108和NRS-271）的抗菌活性。芳香肟酸衍生物11a表现出最高活性，对金黄色葡萄球菌纽曼菌株的最低抑菌浓度（MIC）为0.39-0.78μg/mL。值得注意的是，化合物10b、11和14对五种耐多药金黄色葡萄球菌表现出最强的抗菌活性，MIC值为1.25-3.13μg/mL。这些结果为进一步寻找抗耐多药革兰氏阳性菌感染抗菌候选物的策略优化提供了有用信息。
