Abstrakt
Novel kojyl carbamates of amantadine, rimantadine and oseltamivir were synthesized and assayed to evaluate their antimicrobial activity. The newly compounds were prepared by using EDC/HOBt method at preliminary activation of kojic acid.
The structures of the synthesized kojyl derivatives were confirmed by mp, UV, IR (ATR)umax, ESI-MS. According to the antimicrobial activity studies performed in vitro, kojyl carbamate of rimantadine (4) displayed the highest antibacterial activity (MIC: 31 μg/mL) against two Gram-positive (Staphylococcus aureus, Bacillus subtilis) bacteria.
Moreover, this compound (4) showed about 4-fold better activity against two Gram-negative bacteria tested (Escherichia coli, Pseudomonas aeruginosa). Amongst the examined kojyl carbamates, the rimantadine derivative of kojic acid (4) exhibited the highest antifungal activity (Candida albicans) as well.