CHEMICAL MODIFICATION OF FORTIMICINS

III. PREPARATION OF N-SUBSTITUTED FORTIMICIN A DERIVATIVES

抄録

The 1, 2' or 6'-amino group of fortimicin A was alkylated or acylated and the antimicrobial activities of the derivatives were compared with each other. 2'-N-Substituted fortimicins A were active against the fortimicin A resistant strain which produced AAC(3)-I. AAC(3)-I is the only enzyme which can inactivate fortimicin A. Among the derivatives prepared in the present study, 2'-N-[(S)-4-amino-2-hydroxybutyl]fortimicin A showed stronger activity than fortimicin A. Fortimicins (FM) are pseudodisaccharide aminocyclitol antibiotics produced by Micromonospora