Synthesis and antiphytoviral activity of α-aminophosphonates containing 3, 5-diphenyl-2-isoxazoline as potential papaya ringspot virus inhibitors
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α-Aminophosphonates compounds containing 3,5-diphenyl-2-isoxazoline were synthesized and evaluated for their bioactivity. Seventeen of them showed good bioactivity (protection effect > 50%) in vivo against papaya ringspot virus, while two of them (V29 and V45) exhibited excellent antiviral activity (both 77.8%). In the latter case, the antiviral activity was close to that of antiphytovirucides ningnanmycin and dufulin (both 83.3%) at 500 mg/L. The preliminary structure–activity relationships indicated that the bioactivity was strongly influenced by the substituents.
Keywordsα-Aminophosphonates 3, 5-Diphenyl-2-isoxazoline Synthesis Anti-PRSV activity Structure–activity relationships
This work was financially supported by the National Natural Science Foundation of China (Grant No. 31601675) and the Specialized Research Fund for the Doctoral Program of Education of China (Grant No. 20134404130003). We thank Dr. Xueqin Rao (Department of Plant Pathology, South China Agricultural University) and Dr. Duo Lai (Institute of Fruit Tree Research, Guangdong Academy of Agricultural Sciences, China) for their kind help in screening the compounds for biological activity.
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