单位：[1]Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College[2]Department of Neurology, Beijing Friendship Hospital, Capital Medical University, Beijing, China临床科室神经内科神经内科首都医科大学附属北京友谊医院
Sulbactam, a known beta-lactamase inhibitor, was found to own potent antimicrobial activity against Acinetobacter baumannii in clinical practice. Based on clinical evidence, a series of sulbactam derivatives were designed, synthesized and evaluated for antibacterial activity against Acinetobacter baumannii, taking sulbactam as the lead. Among them, compound 9 exhibited a good antibacterial activity against Acinetobacter baumannii with a MIC value of 4 mu g/mL, slightly lower than that of sulbactam of 1 mu g/mL. Especially, compound 9 displayed outstanding oral pharmacokinetic profiles with a maximum plasma concentration (C-max) of 19.6 mu g/mL and area under the curve (AUC) of 10.8 mu g.h/mL, much higher than those of sulbactam, and thus held the potential of being developed into an oral medication. These results provided the useful information for further structural modification and optimization of its kind, and compound 9 has been selected for the further investigation.
基金：
National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81361138020, 81621064]; CAMS initiative for innovative medicine [2017-12M-1-012]; CAMS Graduate Innovation Fund [2017-1007-19]
第一作者单位：[1]Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College
共同第一作者：
通讯作者：
通讯机构：[1]Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College[*1]Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 10050, China.
推荐引用方式(GB/T 7714)：
YUANSHUAI YANG,SHENG TANG,ZHANDONG LIU,et al.Synthesis and antibacterial evaluation of sulbactam derivatives against Acinetobacter baumannii[J].PHARMAZIE.2018,73(8):433-437.doi:10.1691/ph.2018.8487.
APA：
YUANSHUAI YANG,SHENG TANG,ZHANDONG LIU,YANXIANG WANG,JING PANG...&XI LU.(2018).Synthesis and antibacterial evaluation of sulbactam derivatives against Acinetobacter baumannii.PHARMAZIE,73,(8)
MLA：
YUANSHUAI YANG,et al."Synthesis and antibacterial evaluation of sulbactam derivatives against Acinetobacter baumannii".PHARMAZIE 73..8(2018):433-437
