Application of the Todd-Atherton Synthetic Approach for Chemical Modification of Tetraene Macrolide Antibiotic Lucensomycin

摘要

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.