期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 81, 期 4, 页码 545-552出版社
WILEY
DOI: 10.1111/cbdd.12064
关键词
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.
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