1, 4-ジアミノシクリトール抗生物質の発展

抄録

Several 1, 4-diaminocyclitol-containing aminoglycoside antibiotics have been discovered by four Japanese research groups during the past five years. Fortimicin A, C, D and KG₃ produced by Micromonospora, sporaricin A and C by Saccharopolyspora, istamycin A, B, C and A₂, 2″- N-form-imidoylistamycin A and B by Streptomyces, and dactimicin by Dactylosporangium inhibit strongly the growth of Grampositive and -negative bacteria including most aminoglycosides-resistant strains. These antibiotics are pseudodisaccharides consisting of a diaminosugar and a 1, 4-diaminocyclitol acylated with glycine at the 4-methylamino group. Fortimicin A and some derivatives of this group antibiotics have been evaluated their clinical usefulness. In this review, chemical studies and structure-activty relationships of the 1, 4-diaminocyclitol-aminoglycoside antibiotics are discussed.