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  • Next-generation heterocyclic electrophiles as small-molecule covalent MurA inhibitors [Elektronski vir]
    Ábrányi-Balogh, Péter ...
    Heterocyclic electrophiles as small covalent fragments showed promising inhibitory activity on the antibacterial target MurA (UDP-N-acetylglucosamine 1-carboxyvinyltransferase, EC:2.5.1.7). Here, we ... report the second generation of heterocyclic electrophiles: the quaternized analogue of the heterocyclic covalent fragment library with improved reactivity and MurA inhibitory potency. Quantum chemical reaction barrier calculations, GSH (L-glutathione) reactivity assay, and thrombin counter screen were also used to demonstrate and explain the improved reactivity and selectivity of the N-methylated heterocycles and to compare the two generations of heterocyclic electrophiles.
    Source: Pharmaceuticals [Elektronski vir]. - ISSN 1424-8247 (Vol. 15, iss. 12, art. 1484, 2022, 10 str.)
    Type of material - e-article ; adult, serious
    Publish date - 2022
    Language - english
    COBISS.SI-ID - 132462339

    Link(s):

    https://www.mdpi.com/1424-8247/15/12/1484
    Repository of the University of Ljubljana – RUL
    DOI

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