Abstract: | Structure-activity relationships have been discussed for inhibition of 14C] erythromycin binding to Escherichia coli ribosomes by leucomycin and its acyl derivatives in the light of the Fujita-Ban de novo model. The group contributions of various substituents show that acylation at position 4″ of the mycarose moiety of leucomycin increases affinity for binding of leucomycins to ribosomes. It is also indicated that unlike at position 2' in mycaminose region a free hydroxyl at position 9 of the lactone ring is not important for binding to ribosomes. |