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- W2746700384 abstract "The efficacy of β-lactam antibiotics is threatened by the emergence and global spread of metallo-β-lactamase (MBL) mediated resistance, specifically New Delhi metallo-β-lactamase-1 (NDM-1). By utilization of fragment-based drug discovery (FBDD), a new class of inhibitors for NDM-1 and two related β-lactamases, IMP-1 and VIM-2, was identified. On the basis of 2,6-dipicolinic acid (DPA), several libraries were synthesized for structure-activity relationship (SAR) analysis. Inhibitor 36 (IC50 = 80 nM) was identified to be highly selective for MBLs when compared to other Zn(II) metalloenzymes. While DPA displayed a propensity to chelate metal ions from NDM-1, 36 formed a stable NDM-1:Zn(II):inhibitor ternary complex, as demonstrated by 1H NMR, electron paramagnetic resonance (EPR) spectroscopy, equilibrium dialysis, intrinsic tryptophan fluorescence emission, and UV-vis spectroscopy. When coadministered with 36 (at concentrations nontoxic to mammalian cells), the minimum inhibitory concentrations (MICs) of imipenem against clinical isolates of Eschericia coli and Klebsiella pneumoniae harboring NDM-1 were reduced to susceptible levels." @default.
- W2746700384 created "2017-08-31" @default.
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- W2746700384 date "2017-08-30" @default.
- W2746700384 modified "2023-10-17" @default.
- W2746700384 title "Dipicolinic Acid Derivatives as Inhibitors of New Delhi Metallo-β-lactamase-1" @default.
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- W2746700384 doi "https://doi.org/10.1021/acs.jmedchem.7b00407" @default.
- W2746700384 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5599375" @default.
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- W2746700384 hasPublicationYear "2017" @default.
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