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Synthesis and Antifungal Activity of N-(1,4-Substitued-pyrazole-yl)-heterocyclic Carboxamide Derivatives

WU Zhi-bing,HE Xue-feng,CAI Hua,KUANG Ji-qing,XUE Wei(Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Center for Research and Development of Fine Chemicals,Guizhou University,Guiyang 550025,China)  
[Aims]Pyrazole derivates was a kind of compounds with high and broad-spectrum activity.In order to find heterocyclic carboxamide derivatives with high activity,and this kind of compounds were further studied.[Methods]A series of N-(1,4-disubstituted pyrazole-yl)-heterocyclic carboxamide derivatives were synthesized.All target compounds were bioassayed in vitro against three kinds of phytopathogenic fungi(Gibberella zeae,Fusarium oxysporum,Cytospora mandshurica).[Results]The preliminary results indicated most of the synthesized compounds possessed some antifungal activity against these three tested fungus at 50 mg/L,among which compounds 9j displayed 71.0% inhibition activities against G.zeae at 50 mg/L,and compounds 9l displayed 55.7% inhibition activities against C.mandshurica at 50 mg/L.The molecule structures of the target compounds could be optimized based on the designed compounds.
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