Natural Products as Sources of New Fungicides (I): Synthesis and Antifungal Activity of Acetophenone Derivatives Against Phytopathogenic Fungi
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Abstract
Several series of 45 acetophenone derivatives bearing various alkyl or benzyl substituents were conveniently synthesized and their structures characterized by 1 H and 13 C NMR spectroscopy, HRMS and single‐crystal X‐ray analysis. Their in vitro antifungal activities against a panel of phytopathogenic fungi were evaluated by mycelial growth rate assay. Of them, 12 derivatives (e.g., 3a–c , 4c and 4e ) exhibited more potent antifungal effects on some phytopathogens than a commercial fungicide hymexazol as positive control. In particular, compound 3b with IC 50 values of 10–19 μg/mL was found to be the most active in this series and might be a potential lead structure for further optimization. The preliminary structure–activity relationship (SAR) studies of a series of acetophenones are also discussed.
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