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  • Synthesis, SAR and molecula...
    Antipin, Roman L.; Beshnova, Daria A.; Petrov, Rostislav A.; Shiryaeva, Anna S.; Andreeva, Irina P.; Grigorenko, Vitaly G.; Rubtsova, Maya Yu; Majouga, Alexander G.; Lamzin, Victor S.; Egorov, Alexey M.

    Bioorganic & medicinal chemistry letters, 04/2017, Letnik: 27, Številka: 7
    Journal Article

    Display omitted The novel classes of acylated phenoxyanilide and thiourea compounds were investigated for their ability to inhibit TEM type β-lactamase enzyme. Two compounds 4g and 5c reveal the inhibition potency in micromolar range and show their action by non-covalent binding in the vicinity of the TEM-171 active site. The structure activity relationship around carbon chain length and different substituents in ortho- and para-positions of acylated phenoxyanilide as well as molecular modelling study has been performed.