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 KG
3 produced by
Micromonospora, sporaricin A and C by
Saccharopolyspora, istamycin A, B, C and A
2, 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.
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