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Appl Environ Microbiol. 1969 August; 18(2): 159-165
Copyright © 1969 American Society for Microbiology. All Rights Reserved.

Antibacterial Activity of 2'-Esters of Erythromycin

Biological Development, Abbott Laboratories, Scientific Divisions, North Chicago, Illinois 60064

ABSTRACT

The effect of esterification at the 2'-position of desosamine on the antibacterial activity of erythromycin was investigated by determining the bacteriostatic and bactericidal activities of erythromycin and a number of its 2'-esters on S. aureus and relating these activities to the hydrolysis rates of the esters. These studies, together with comparison of the inhibition of protein synthesis in a cell-free system isolated from S. aureus, lead to the conclusion that 2'-esters of erythromycin are inactive until hydrolyzed. Loss of activity appears to result from inability of erythromycin esters to bind to bacterial ribosomes and thus inhibit synthesis of protein.