N-(取代吡啶基)-1-甲基(苯基)-3-(三氟甲基)-1H-吡唑-4-甲酰胺衍生物的合成及抑菌活性。
Synthesis and antifungal activity of N-(substituted pyridinyl)-1-methyl(phenyl)-3-(trifluoromethyl)-1H-pyrazole-4-carboxamide derivatives.
机构信息
State Key Laboratory Breeding Base of Green Pesticides and Agricultural Bioengineering, Key Laboratory of Green Pesticides and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, China.
出版信息
Molecules. 2012 Nov 30;17(12):14205-18. doi: 10.3390/molecules171214205.
A series of N-(substituted pyridinyl)-1-methyl(phenyl)-3-trifluoromethyl-1H-pyrazole-4-carboxamide derivatives were synthesized. All target compounds were characterized by spectral data (¹H-NMR, ¹³C-NMR, IR, MS) and elemental analysis and were bioassayed in vitro against three kinds of phytopathogenic fungi (Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica). The results showed that some of the synthesized N-(substituted pyridinyl)-1-methyl-3-trifluoromethyl-1H-pyrazole-4-carboxamides exhibited moderate antifungal activities, among which compounds 6a, 6b and 6c displayed more than 50% inhibition activities against G. zeae at 100 µg/mL, which was better than that of the commercial fungicides carboxin and boscalid.
合成了一系列 N-(取代吡啶基)-1-甲基(苯基)-3-三氟甲基-1H-吡唑-4-甲酰胺衍生物。所有目标化合物均通过光谱数据（1H-NMR、13C-NMR、IR、MS）和元素分析进行了表征，并在体外对三种植物病原菌（禾谷镰孢菌、尖孢镰刀菌、杨树溃疡病菌）进行了生物测定。结果表明，部分合成的 N-(取代吡啶基)-1-甲基-3-三氟甲基-1H-吡唑-4-甲酰胺具有中等的抗真菌活性，其中化合物 6a、6b 和 6c 在 100 µg/mL 时对禾谷镰孢菌的抑制活性超过 50%，优于商品化杀菌剂咯菌腈和苯醚甲环唑。
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