Binding Studies on Modified Vancomycin

Abstract

Binding studies were carried out on a vancomycin derivative to examine its potential bactericidal activity. Of particular interest was the effect of dimethylation of the amino group at the N-terminus of vancomycin on the binding ability of the antibiotic to bacterial cell-wall peptide analogues, namely Ac-D-Ala-D-Ala and Ac₂-L-Lys-D-Ala-D-Ala. Reductive methylation was carried out with sodium cyanoborohydride and formaldehyde, and the binding constants of the vancomycin derivative with the peptides were measured by ultraviolet difference spectroscopy.