Abstract
Starting from the mucohalogen acids 1a and b 5-hydroxy-2(5 H)-furanones 2a– h have been prepared and tested. These novel 4-amino-5-hydroxy 2(5 H)-furananones have shown a broad antibiotic activity against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 in the micromolar range. A one step synthesis from mucohalogen acids towards the antibacterials 2a– h was developed, in which the target was obtained from 1a and b under reflux in toluene in presence of a catalytic amount of sulfuric acid. The derivatives 2b and c displayed a MIC and MBC of 4/8 μg/ml, against Staphylococcus aureus with a selectivity towards the resistant strains.
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