| 摘要 |
<p>Kanamycin derivs. of formula (I) and their acid addn. salts are new. In (I) R is hydroxy or H. R1 is H or a gp. of formula -CO.CH(OH).(CH2)n.NH2(A). n is 1-3. R2 is H or methyl. With the proviso that R2 is not methyl when R is H. (I) are antibacterials with good activity against a wide range of species, including those resistant to kanamycin. The intravenous LD50 in mice is 25-100 mg. per kg, and (I) are formulated conventionally for an oral dose of 0.1-1g per day; intramuscular dose of 0.05-0.5g (1-4 times per day), or as an ointment contg. 0.5-5%(I). 8 cpds. are specifically claimed e.g. 1-N-((S)-4-amino- 2-hydroxybutyryl)- 5,3',4'-trideoxykanamycin B (Ia) and its 5,3',4',6"-tetradeoxy analogue; 5,3',4',6"-tetradeoxykanamycin B (Ib) or 5,3',4'-trideoxy- 6'-N-methylkanamycin B (Ib).</p> |
