Application of the Todd–Atherton synthetic approach for chemical modification of tetraene macrolide antibiotic lucensomycin

Abstract

Lucensomycin, tetraene macrolide antibiotic, has been chemically modified with dialkyl(diaryl) phosphites under conditions of the Todd–Atherton reaction. The reaction has yielded the corresponding dialkyl-(diaryl) amidophosphate derivatives of the antibiotic. Physico-chemical properties of the prepared derivatives as well as their toxicity and antifungal activity towards a series of pathogenic Candida yeast-like fungi have been studied. The automated decision-making information system for selection of highly efficient antibiotics has been described.