The synthesis and antistaphylococcal activity of dehydroabietic acid derivatives: Modifications at C-12
The synthesis and antistaphylococcal activity of dehydroabietic acid derivatives: Modifications at C-12
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脱氢松香酸衍生物的合成和抗葡萄球菌活性：C-12 修饰
DOI：
10.1016/j.bmcl.2016.10.018
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发表时间：
2016-11-15
影响因子：
2.7
通讯作者：
Cui, Yong-Mei
中科院分区：
文献类型：
--
作者：
Liu, Ming-Liang;Pan, Xue-Ying;Cui, Yong-Mei
合成了一系列脱氢松油酸的12-肟醚和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5株耐多药菌株(NRS-1、NRS-70、NRS-100、NRS-108和NRS-271)的抗菌活性。芳香族肟酸酯类化合物11a对金黄色葡萄球菌的MIC为0.39~0.78 mU/m L，活性最高。值得注意的是，化合物10b、11和14对5株耐多药金黄色葡萄球菌显示出最强的抗菌活性，其MIC值为1.25-3.13微克/毫升。这些结果为进一步的战略优化提供了有用的信息，以寻找对抗多重耐药革兰氏阳性菌感染的候选抗菌药物。(C)2016爱思唯尔有限公司。保留所有权利。
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 0.39-0.78 mu g/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 1.25-3.13 mu g/mL. These results offered useful information for further strategic optimization in search of the antibacterial candidates against infection of multidrug-resistant Gram-positive bacteria. (C) 2016 Elsevier Ltd. All rights reserved.