Studies on viomycin. IX. Amino acid derivatives of viomycin.

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Abstract
The limited acylations of I [a viomycin derivative] on the 2 amino functions of .beta.-lysine residue with protected amino acid active esters followed by de-protection by catalytic hydrogenolyses resulted in N1-amino acid acylated viomycins. Limited carbobenzoxylation followed by reaction with dicarbobenzoxylysine active ester and decarbobenzoxylation gave N6-acylated product VI. Antimicrobial assay of the above obtained derivatives show that neutral amino acid derivatives of I have reduced potencies while basic amino acid derivatives possess almost the similar potencies with I in vitro and in vivo tests. One of the probable reasons for the importance of the 2 free amino functions of .beta.-lysine residue for the exhibition of the [antibacterial] potency of I is concluded to be due to their basicity.

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