1-Substd. amino-aminoglycosyl diaminocyclitol derivs. - broad spectrum antibiotics prepd. e.g. by reductive alkylation of gentamicins

摘要

derivs. (I) of gentamicin A, B1, C1, C1a, C2a, C2b, sisomicin; verdamicin; tobramycin; antibiotics G-418, 66-40b, 66-4OD, J1-20A, J1-20B, G-52; mutamicins 1,2,4,5 or 6, substd. on the 1-N atom by CH2X or COZ (where X = H, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, aminoalkyl, N-alkyl aminoalkyl, aminohydroxyalkyl, N-alkyl aminohydroxyalkyl, phenyl, benzyl or tolyl; aliphatic gps. have is not 7C and hydroxy and amino when both present are on separate C atoms; Z = X, provided that COZ is other than 5-3-amino-2-hydroxypropionyl, S-4-amino-2-hydroxybutyryl or (only for tobramycin) S-5-amino-2-hydroxyvaleryl) and their acid addn. salts are broad-spectrum antibacterials active against some strains resistant to the parent 1-amino cpds.; some are also antiprotozoals, antiamoebics and anthelmintics. They are be used therapeutically in human or veterinary medicine (e.g. 1-N-ethylsisomicin and 1-N-ethylverdamicin are useful for controlling mastitis, and Salmonella infections in cats) or as surface disinfectants. (I; COZ) are intermediates for (I; CH2X).