Synthesis and biological evaluation of arabinose 5-phosphate mimics modified at position five

• We designed and synthesised a set of new Ara-5P analogues, modified at position 5.
• We tested the affinity of the synthesised compounds by STD-NMR spectroscopy studies.
• The synthesised compounds were studied in vivo on P. aeruginosa and E. coli strains.
• None of the compounds was active, either in vivo or on isolated API.

A set of new metabolically stable arabinose 5-phosphate analogues possessing phosphate mimetic groups at position 5 was synthesised. Their ability to interact with arabinose 5-phosphate isomerase from Pseudomonas aeruginosa was evaluated by STD-NMR studies. The synthesised compounds were also characterised for their activity in vivo on P. aeruginosa and Escherichia coli strains. Unfortunately, none of the synthesised compounds was able neither to bind API nor to inhibit bacterial growth.

Figure optionsDownload as PowerPoint slide