Antibacterial activity of xylose-derived LpxC inhibitors – Synthesis, biological evaluation and molecular docking studies

LpxC inhibitors represent a promising class of novel antibiotics selectively combating Gram-negative bacteria. In chiral pool syntheses starting from D- and L-xylose, series four 2r,3c,4t-configured C-furanosidic was obtained. The synthesized hydroxamic acids were tested for antibacterial inhibitory activity, the acquired biological data compared with those previously C-furanosides, molecular docking studies performed to rationalize observed structure-activity relationships. Additionally, bacterial uptake susceptibility efflux pump systems investigated most stereoisomers.