Synthesis and antibacterial activities of 1-N [(S)-.OMEGA.-amino-2-hydroxyalkyl] kanamycin a derivatives.

Abstract

Four 1-N-aminohydroxy-alkyl derivatives of kanamycin A were prepared and their in vitro activities against aminoglycoside-sensitive and aminoglycoside-resistant organisms were compared with amikacin. 1-N-[(S)-4-Amino-2-hydroxybutyl] kanamycin A (Fig. 1, compound 2, code no. UK-18, 892) was equipotent to amikacin in all these tests and in mouse protection studies.