In Vitro Antifungal Activity of Sanguinarine and Chelerythrine Derivatives against Phytopathogenic Fungi

摘要

In order to understand the antifungal activity of some derivatives of sanguinarine (>S) and chelerythrine (>C) and their structure-activity relationships, sixteen derivatives of >S and >C were prepared and evaluated for in vitro antifungal activity against seven phytopathogenic fungi by the mycelial growth rate method. The results showed that >S, >C and their 6-alkoxy dihydro derivatives >S1–>S4, >C1–>C4 and 6-cyanodihydro derivatives >S5, >C5 showed significant antifungal activity at 100 µg/mL against all the tested fungi. For most tested fungi, the median effective concentrations of >S, >S1, >C and >C1 were in a range of 14–50 µg/mL. The structure-activity relationship showed that the C=N⁺ moiety was the determinant for the antifungal activity of >S and >C. >S1–>S5 and >C1–>C5 could be considered as the precursors of >S and >C, respectively. Thus, the present results strongly suggested that >S and >C or their derivatives >S1–>S5 and >C1–>C5 should be considered as good lead compounds or model molecules to develop new anti-phytopathogenic fungal agents.