Synthesis and Biological Activities of Diosgenin-Triazole Conjugates with a 1,3-Dipolar Cycloaddition Reaction

A novel series of diosgenin-triazole conjugates (10a–d, 11a–c, 12a–c, 13a–c) was designed and synthesized as antifungal agents by using a 1,3-dipolar cycloaddition reaction in the presence of a Cu(I) catalyst. All the title compounds were characterized by 1H NMR, 13C NMR, and Q-TOF-MS. Results of preliminary antifungal tests against seven human pathogenic fungi in vitro revealed that half of the target compounds exhibited moderate or even better antifungal activities against Y0109 and C. albicans SC5314 species. Compound 10d showed excellent antifungal activities toward C. albicans Y0109 and C. albicans SC5314 than itraconazole, with MIC80 value of 1 μg/mL, respectively.