Synthesis and antifungal activity of N-aryl-substituted pimaricin derivatives

Reactions of the tetraene macrolide antibiotic pimaricin with 1-fluorobenzenes resulted in the formation of N-aryl-substituted derivatives. The physicochemical and biological properties of the synthesized pimaricin derivatives were studied. The N-aryl-substituted pimaricin derivatives showed high antifungal activity against a broad spectrum of test cultures. The biological studies showed that the acute toxicity (LD₅₀) of the obtained pimaricin derivatives was half that of the starting antibiotic.