1246633-35-1Relevant academic research and scientific papers
Synthesis and antimicrobial properties of cyclic fluorodiamines containing boronate esters
Zhu, Diya,Hunter, Carmanah D.,Baird, Samuel R.,Davis, Bradley R.,Bos, Allyson,Geier, Stephen J.,Vogels, Christopher M.,Decken, Andreas,Gray, Christopher A.,Westcott, Stephen A.
, (2017)
Eight new aminoboron compounds derived from primary diamines and the pinacol-protected product of 3-fluoro-2-formylphenylboronic acid have been prepared and characterized fully. Reactions proceed to give the corresponding cyclic products arising via initial aldimine formation followed by a secondary hydroamination step. One compound contains a pendant amine group which was used to make a novel boron-containing Schiff base ligand along with the corresponding zinc(II) metal complex. All compounds were tested for their initial antimicrobial activities against a number of fungi and bacteria.
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.
Imidazole-containing condensed tricyclic compound and application thereof
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Paragraph 0204, (2018/03/01)
The invention discloses an imidazole-containing condensed tricyclic compound adopting the structure as shown in the formula (I) or pharmaceutically acceptable salts, stereisomers or prodrug molecules thereof. The imidazole-containing condensed tricyclic compound has the IDO1 activity regulation function, can enhance T-cell activation through blocking immune checkpoints IDO1, is used for treating IDO1-mediated immunosuppression, and therefore, can become an effective medicine for treating malignant tumors. When used together with checkpoint protein anti-body drugs or other anti-cancer drugs, the imidazole-containing condensed tricyclic compound can enhance the anti-cancer effect. Meanwhile, the imidazole-containing condensed tricyclic compound has the potential of effectively treating IDO1 abnormity related immunosuppressive diseases and has a high application value.
