cas 94838-88-7, 2-FORMYL-4,5-METHYLENEDIOXYPHENYLBORONIC ACID | Articles data ｜lookchem

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94838-88-7

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Discovery of 3-aryl substituted benzoxaboroles as broad-spectrum inhibitors of serine- and metallo-β-lactamases
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.
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
(2021)
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Chemical Properties

Melting Point: 231-233 °C
Boiling Point: 434.3 °C at 760 mmHg
Flash Point:216.5 °C
Density: 1.49 g/cm³
Storage Temp.:2-8°C
Vapor Pressure: 2.59E-08mmHg at 25°C
Refractive Index: 1.598
PKA: 8.13±0.20(Predicted)
PSA: 75.99000
LogP: -1.09240

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