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Publication Detail
Triazole-substituted phenylboronic acids as tunable lead inhibitors of KPC-2 antibiotic resistance
  • Publication Type:
    Journal article
  • Authors:
    Zhou J, Stapleton P, Xavier-Junior FH, Schatzlein A, Haider S, Healy J, Wells G
  • Publisher:
    Elsevier BV
  • Publication date:
  • Journal:
    European Journal of Medicinal Chemistry
  • Volume:
  • Article number:
  • Status:
  • Language:
  • Keywords:
    Antimicrobial resistance (AMR) KPC-2, Phenylboronic acids, SAR
  • Notes:
    © 2022 The Authors. Published by Elsevier Masson SAS. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
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, respectively) 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 additional property of the compounds that could be tuned to optimize the target interaction and/or the physicochemical 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.
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