Natural Products as Sources of New Fungicides (I): Synthesis and Antifungal Activity of Acetophenone Derivatives Against Phytopathogenic Fungi

作者：Ma, Ya-Tuan; Fan, Hua-Fang; Gao, Yu-Qi; Li, He; Zhang, An-Ling^*; Gao, Jin-Ming

来源：Chemical Biology & Drug Design, 2013, 81(4): 545-552.

DOI：10.1111/cbdd.12064

• 2
• 4-dihydroxy-5-methylacetophenone
• acetophenone derivatives
• antifungal activity
• natural products
• structureactivity relationship

Several series of 45 acetophenone derivatives bearing various alkyl or benzyl substituents were conveniently synthesized and their structures characterized by 1H and 13C 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., 3ac, 4c and 4e) exhibited more potent antifungal effects on some phytopathogens than a commercial fungicide hymexazol as positive control. In particular, compound 3b with IC50 values of 1019g/mL was found to be the most active in this series and might be a potential lead structure for further optimization. The preliminary structureactivity relationship (SAR) studies of a series of acetophenones are also discussed.

• 出版日期2013-4
• 单位西北农林科技大学