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- Title
Natural Products as Sources of New Fungicides (I): Synthesis and Antifungal Activity of Acetophenone Derivatives Against Phytopathogenic Fungi.
- Authors
Ma, Ya ‐ Tuan; Fan, Hua ‐ Fang; Gao, Yu ‐ Qi; Li, He; Zhang, An ‐ Ling; Gao, Jin ‐ Ming
- Abstract
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., 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 IC50 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.
- Subjects
ACETOPHENONE derivatives; FUNGICIDES; ANTIFUNGAL agents; PHYTOPATHOGENIC fungi; ALKYL compounds; BENZYL compounds
- Publication
Chemical Biology & Drug Design, 2013, Vol 81, Issue 4, p545
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12064