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

Ma YaTuan | Zendy; Fan HuaFang | Zendy; Gao YuQi | Zendy; Li He | Zendy; Zhang AnLing | Zendy; Gao JinMing | Zendy

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

Author(s) -

Ma YaTuan,

Fan HuaFang,

Gao YuQi,

Li He,

Zhang AnLing,

Gao JinMing

Publication year - 2013

Publication title -

chemical biology and drug design

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.59

H-Index - 77

eISSN - 1747-0285

pISSN - 1747-0277

DOI - 10.1111/cbdd.12064

Subject(s) - acetophenone , fungicide , mycelium , antifungal , chemistry , stereochemistry , structure–activity relationship , lead compound , in vitro , organic chemistry , biology , biochemistry , microbiology and biotechnology , botany , catalysis

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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