Related Experiment Video
Updated: Jun 4, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
2-Carboxyquinoline Boronic Acids as Highly Potent KPC Inhibitors
Zheng Ma1, Ge Cui1, Lijie Dou1
1State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, Frontiers Science Center for Materiobiology and Dynamic Chemistry, Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism, School of Pharmacy, East China University of Science and Technology, Shanghai, 200237, P.R. China.
Abstract:
The expression of Klebsiella pneumoniae carbapenemase (KPC), a type of carbapenem-hydrolyzing β-lactamase, in Gram-negative bacteria has caused significant bacterial resistance to carbapenems, the antibiotic of last resort. Herein, we describe the discovery of 2-carboxyquinoline boronic acids as inhibitor of KPC. We have identified fluoro-substituted carboxyquinoline boronic acids 1 e as the most potent inhibitor, with an IC50 of 8.3 nM for KPC-2, while this compound is significantly less efficient at reducing the activity of other β-lactamases. This compound proved to have low cytotoxicity towards mammalian cells, as well as low haemolysis and antibacterial activity. However, 1 e potentiated the efficacy of β-lactam antibiotics (e. g., meropenem and ceftazidime) against KPC-2-expressing resistant Klebsiella pneumonia by up to 256-fold.
More Related Videos
Related Concept Videos
Inhibition of Cdk Activity
Gene Regulation in Microbial Communities: Quorum Sensing
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Indirect-Acting Cholinergic Agonists: Mechanism of Action
Reversible inhibitors like edrophonium bind to a specific part of the enzyme called the anionic catalytic site. They form noncovalent bonds, which means they are not strongly attached to the enzyme. This creates a temporary and less stable enzyme–inhibitor complex,...
Cofactors and Coenzymes
Carbocations

