Studies on Viomycin. IX. Amino Acid Derivatives of Viomycin

概要

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The limited acylations of I on the two amino functions of β-lysine residue with protected amino acid active esters followed by de-protection by catalytic hydrogenolyses resulted N_1-amino acid acylated viomycins. While, the limited carbobenzoxylation followed by the reaction with dicarbobenzoxylysine active ester and the decarbobenzoxylation gave N_6-acylated product VI. Antimicrobial assay of the above obtained derivatives result 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. Thus, one of the provable reason for the importance of the two free amino functions of β-lysine residue for the exhibition of the potency of I is concluded to be due to their basicity.
公益社団法人日本薬学会の論文
1976-06-25