Synthesis and Antifungal and Antiviral Activity of N-Benzyl Derivatives of the Tetraene Macrolide Antibiotic Lucensomycin

Resumo

Reductive amination of the tetraene macrolide antibiotic lucensomycin by para-substituted benzaldehydes and cyanoborohydride formed its N-benzyl derivatives. The physicochemical, medical, and biological properties of the obtained pimaricin derivatives were studied. Biological tests showed that the N-benzyl lucensomycin derivatives possessed high antifungal and antiviral activity. Pharmacological tests showed that the acute toxicity (LD₅₀) of the synthesized lucensomycin derivatives was six times less than that of the starting antibiotic.