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Natural Products as Sources of New Fungicides (I): Synthesis and Antifungal Activity of Acetophenone Derivatives Against Phytopathogenic Fungi.
- Source :
-
Chemical Biology & Drug Design . Apr2013, Vol. 81 Issue 4, p545-552. 8p. 3 Diagrams, 2 Charts. - Publication Year :
- 2013
-
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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 17470277
- Volume :
- 81
- Issue :
- 4
- Database :
- Academic Search Index
- Journal :
- Chemical Biology & Drug Design
- Publication Type :
- Academic Journal
- Accession number :
- 86407377
- Full Text :
- https://doi.org/10.1111/cbdd.12064