Hydrophosphoryl derivatives of tetramycin B: Design, synthesis, biological activity and development of intellectual computer system

Abstract

The reactions of tetraene macrolide antibiotic, tetramycin B, with aromatic aldehydes and hypophosphorous acid under conditions of Kabachnik-Fields method result in formation of its hydrophosphoryl derivatives. The physicochemical, medical, and biological properties of the obtained tetramycin B derivatives were studied. Pharmacological tests showed that the acute toxicity (LD₅₀) of the synthesized hydrophosphoryl derivatives was 6-7 times less than that of the starting antibiotic. Biological tests showed that the hydrophosphoryl derivatives of tetramycin B possessed high antifungal and antiviral activity.

Graphical Abstract

Keywords:

• Tetramycin B
• Kabachnik-Fields reaction
• biological activity
• toxicity