含芳基四唑链的酰化物衍生物的合成及其抗菌活性
Synthesis and antibacterial activities of acylide derivatives bearing an aryl-tetrazolyl chain.
作者信息
Shan Ling-Xing, Sun Ping-Hua, Guo Bao-Qin, Xu Xing-Jun, Li Zhi-Qiang, Sun Jia-Zhi, Zhou Shu-Feng, Chen Wei-Min
机构信息
Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, People's Republic of China.
Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, People's Republic of China ; College of Pharmacy, University of South Florida, Tampa, FL, USA.
出版信息
Drug Des Devel Ther. 2014 Sep 24;8:1515-25. doi: 10.2147/DDDT.S65673. eCollection 2014.
Seventeen acylides bearing an aryl-tetrazolyl alkyl-substituted side chain were synthesized, starting from clarithromycin, via several reactions including hydrolysis, acetylating, esterification, carbamylation, and Michael addition. The structures of all new compounds were confirmed by (1)H nuclear magnetic resonance spectroscopy, (13)C nuclear magnetic resonance spectroscopy, and mass spectrometry. All these synthesized acylides were evaluated for in vitro antimicrobial activities against gram-positive pathogens (Staphylococcus aureus, Staphylococcus epidermidis) and gram-negative pathogens (Pseudomonas aeruginosa, Escherichia coli), using the broth microdilution method. Results showed that compounds 10 e, 10 f, 10 g, 10 h, 10 o have good antibacterial activities.
以克拉霉素为起始原料，通过水解、乙酰化、酯化、氨甲酰化和迈克尔加成等一系列反应，合成了17种带有芳基 - 四唑基烷基取代侧链的酰化物。所有新化合物的结构均通过氢核磁共振光谱、碳核磁共振光谱和质谱得到确证。采用肉汤微量稀释法，对所有合成的酰化物针对革兰氏阳性病原体（金黄色葡萄球菌、表皮葡萄球菌）和革兰氏阴性病原体（铜绿假单胞菌、大肠杆菌）的体外抗菌活性进行了评估。结果表明，化合物10e、10f、10g、10h、10o具有良好的抗菌活性。
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