Design, Synthesis and Antifungal Activity of Phloroglucinol Derivatives

Authors：Yang, Meizhu; Lai, Weihong; Li, Junjian; Ye, Lianbao^*

Source：PHARMACEUTICAL CHEMISTRY JOURNAL, 2022, 56(3): 356-360.

DOI：10.1007/s11094-022-02651-w

• antimicrobials
• acyl groups
• Trichophyton rubrum
• Trichophyton mentagrophytes
• lead compounds

Phloroglucinols of Dryopteris fragrans (L.) Schott plant show strong antifungal activity. In previous work, we isolated a wide range of phloroglucinols from the plant and found that pseudoaspidinol of D. fragrans and its structural modifications (methylphloroglucinol derivatives) showed stronger antifungal activity and confirmed that the butyryl group of these compounds accounted for this activity. In this study, we designed a series of phloroglucinol derivatives (A1-A9) and methylphloroglucinol derivatives (B1-B9) by introducing acyl groups with diverse carbon numbers in the C-2 position, synthesized these compounds, and evaluated the anti-dermatophyte activity of compounds A1-A5 and B1-B5 on Trichophyton rubrum and Trichophyton mentagrophytes fungal species. The results showed that compound A5 exhibited the strongest activity. These compounds can be used as leads for the development of new antifungal agents.

• Institution
  广东药学院; 广州医学院