SYNTHESIS OF 2''-AMINO-2''-DEOXYARBEKACIN AND ITS ANALOGS HAVING POTENT ACTIVITY AGAINST METHICILLIN-RESISTANT STAPHYLOCOCCUS-AUREUS

Based on our studies on the enzymatic modifications of arbekacin by me thicillin-resistant Staphylococcus aureus (MRSA), replacement of the 2 ''-hydroxyl group by an amino group in arbekacin was designed to synth esize derivatives that would be active against MRSA. 2''-Amino-2''-deo xyarbekacin and five analogs were synthesized starting from dibekacin. Among them, 2''-amino-2''-deoxyarbekacin and the 5-epiamino analog sh owed excellent antibacterial activities against not only MRSA but also Gram-negative bacteria including Pseudomonas, and lower toxicities th an arbekacin.