摘要 |
<p>The invention provides 5-deoxy-5,5-difluoro derivatives of aminoglycoside antibiotics of neamine, kanamycin A, kanamycin B, gentamicin and seldomycin, each synthesized as a novel compound, and also 1-N-( alpha -hydroxy- omega -aminoalkanoyl) derivatives synthesized from the newly obtained 5-deoxy-5,5-difluorokanamycins A and B and analogs thereof. The 5-deoxy-5,5-difluoro derivatives thus obtained have antibacterial activities superior or substantially equivalent to those of the amino-glycoside antibiotics from which they are derived and further have a remarkably improved median lethal dose (LD50) when intravenously administered to mice and a remarkably reduced toxicity on mammals.</p> |
申请人 |
ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI, TOKIO/TOKYO, JP |
发明人 |
TAKEUCHI, TOMIO, 5-CHOME, SHINAGAWA-KU, TOKYO 141, JP;UMEZAWA, SUMIO, SHINJUKU-KU, TOKYO 160, JP;TSUCHIYA, TSUTOMU, MIDORI-KU, YOKOHAMA-SHI, KANAGAWA 227, JP;SHITARA, TETSUO, NAKAHARA-KU, KAWASAKI-SHI, KANAGAWA 211, JP;FUKATSU, SHUNZO, SHINJUKU-KU, TOKYO 162, JP;UMEMURA, EIJIRO, CHIGASAKI-SHI, KANAGAWA 253, JP |