Zhou, Jingyuan published the artcileTriazole-substituted phenylboronic acids as tunable lead inhibitors of KPC-2 antibiotic resistance, Application of 2-(5-(Bromomethyl)-2-fluorophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, the publication is European Journal of Medicinal Chemistry (2022), 114571, database is CAplus and MEDLINE.
Inhibition of β-lactamases is a promising strategy to overcome antimicrobial resistance to commonly used β-lactam antibiotics. Boronic acid derivatives have proven to be effective inhibitors of β-lactamases due to their direct interaction with the catalytic site of these enzymes. We synthesized a series of phenylboronic acid derivatives and evaluated their structure-activity relationships as Klebsiella pneumoniae carbapenemase (KPC-2) inhibitors. We identified potent KPC-2 inhibitors 2e & 6c (Ki = 0.032 μM and 0.038 μM, resp.) that enhance the activity of cefotaxime in KPC-2 expressing Escherichia coli. The measured acid dissociation constants (pKa) of selected triazole-containing phenylboronic acids was broad (5.98-10.0), suggesting that this is an addnl. property of the compounds that could be tuned to optimize the target interaction and/or the physicochem. properties of the compounds These findings will help to guide the future development of boronic acid compounds as inhibitors of KPC-2 and other target proteins.
European Journal of Medicinal Chemistry published new progress about 1256360-47-0. 1256360-47-0 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Boronic acid and ester,Benzyl bromide,Benzene,Boronate Esters,Boronic Acids,Boronic acid and ester, name is 2-(5-(Bromomethyl)-2-fluorophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, and the molecular formula is C25H23NO4, Application of 2-(5-(Bromomethyl)-2-fluorophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane.
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