Horizon in 1,4-Diaminocyclitol-Aminoglycoside Antibiotics

Abstract

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 Gram-positive and -negative bacteria including most aminoglycosides-resistant strains. These antibiotics are pseudodisaccharides consisting of a diaminosugar and a 1,4-diamino-cyclitol 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. © 1982, The Society of Synthetic Organic Chemistry, Japan. All rights reserved.