871126-15-7Relevant articles and documents
Discovery of 3-aryl substituted benzoxaboroles as broad-spectrum inhibitors of serine- and metallo-β-lactamases
Yan, Yu-Hang,Li, Zhao-Feng,Ning, Xiang-Li,Deng, Ji,Yu, Jun-Lin,Luo, Yubin,Wang, Zhenling,Li, Guo,Li, Guo-Bo,Xiao, You-Cai
supporting information, (2021/04/12)
The production of β-lactamases represents the main cause of resistance to clinically important β-lactam antibiotics. Boron containing compounds have been demonstrated as promising broad-spectrum β-lactamase inhibitors to combat β-lactam resistance. Here we report a series of 3-aryl substituted benzoxaborole derivatives, which manifested broad-spectrum inhibition to representative serine-β-lactamases (SBLs) and metallo-β-lactamases (MBLs). The most potent inhibitor 9f displayed an IC50 value of 86 nM to KPC-2 SBL and micromolar inhibitory activity towards other tested enzymes. Cell-based assays further revealed that 9f was able to significantly reduce the MICs of meropenem in clinically isolated KPC-2-producing bacterial strains and it showed no apparent toxicity in HEK293T cells.
Method for preparing 3-fluorine-2-aldehyde phenylboronic acid
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Paragraph 0017; 0018; 0019, (2017/02/09)
The invention discloses a method for preparing 3-fluorine-2-aldehyde phenylboronic acid. Starting from 3-fluorine phenylboronic acid, tripolymer is formed after heating reflux in methylbenzene or heptane and dehydration, then a lithium reagent is added to