The preparations of 4-N-glycyllysinomicin and several 4-N-aminoacyl derivatives of compounds prepared from lysinomicin are presented. The new substances have lower antimicrobial activities than the original 4-N-unsubstituted lysinomicin derivatives. This result indicates that the structure-activity relationship observed with fortimicin A and fortimicin B does not apply to the lysinomicin derivatives studied.