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Antibacterial activity of xylose-derived LpxC inhibitors - Synthesis, biological evaluation and molecular docking studies.
Dreger, Alexander Hoff, Katharina Agoglitta, Oriana Hotop, Sven-Kevin Heisig, Peter Kirchmair, Johannes Holl, Ralph
Dreger, Alexander
Hoff, Katharina
Agoglitta, Oriana
Hotop, Sven-Kevin
Heisig, Peter
Kirchmair, Johannes
Holl, Ralph
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2020-12-31
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Abstract
LpxC inhibitors represent a promising class of novel antibiotics selectively combating Gram-negative bacteria. In chiral pool syntheses starting from D- and L-xylose, a series of four 2r,3c,4t-configured C-furanosidic LpxC inhibitors was obtained. The synthesized hydroxamic acids were tested for antibacterial and LpxC inhibitory activity, the acquired biological data were compared with those of previously synthesized C-furanosides, and molecular docking studies were performed to rationalize the observed structure-activity relationships. Additionally, bacterial uptake and susceptibility to efflux pump systems were investigated for the most promising stereoisomers.
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Bioorg Chem. 2020 Dec 31;107:104603. doi: 10.1016/j.bioorg.2020.104603. Epub ahead of print.
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en
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1090-2120
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Attribution-NonCommercial-NoDerivatives 4.0 International