| Literature DB >> 28237762 |
Roman L Antipin1, Daria A Beshnova2, Rostislav A Petrov3, Anna S Shiryaeva3, Irina P Andreeva3, Vitaly G Grigorenko3, Maya Yu Rubtsova3, Alexander G Majouga4, Victor S Lamzin2, Alexey M Egorov3.
Abstract
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.Entities:
Keywords: Acylated phenoxyaniline; Molecular docking; TEM type β-lactamase; Thiourea; β-Lactamase inhibitors
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Year: 2017 PMID： 28237762 DOI： 10.1016/j.bmcl.2017.02.025
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823