Synthesis and antifungal activity of polycyclic pyridone derivatives with anti-hyphal and biofilm formation activity against Candida albicans

Thirty-five pyridone derivatives were synthesized, with derivatization conducted on polycyclic pyridone scaffolds, including cis-or trans-oxydecalin and other cyclic structures, by domino-Knoevenagel-electrocyclic reactions. The anti-fungal activities of the synthesized compounds were tested against Candida albicans. Ten compounds inhibited hyphal formation without inhibiting growth. Pyridones with anti-hyphal formation activity (4c, 6d, 12a and 12c) were tested for their ability to inhibit biofilm formation. Compound 6d showed both antihyphal and biofilm inhibition activity.

Automated summary

Thirty-five pyridone derivatives were synthesized using domino-Knoevenagel-electrocyclic reactions on various polycyclic pyridone scaffolds. These compounds were tested for anti-fungal activities against Candida albicans. Among them, compound 6d showed both anti-hyphal and biofilm inhibition activities.