【摘要】 根据药物分子设计的活性基团组合原理,通过在1,2,4-三唑环的5位引入吡啶基,同时在4位芳基亚甲氨基的苯环上引入氟或三氟甲基,设计合成了一系列含氟、吡啶和哌嗪基团的1,2,4-三唑Mannich碱和双Mannich碱类化合物.通过核磁共振氢谱（¹H NMR）、碳谱(¹³C NMR)和元素分析确证了目标化合物的结构.生物活性测试结果表明,部分化合物对油菜具有一定的除草活性;化合物2a,2d和2f（50 mg/L）对苹果轮纹病菌表现出较好的抑制活性,与对照药三唑酮活性相当;化合物2a,2b,2d和2i（180 mg/L）对酮醇酸还原异构酶（KARI酶）表现出了显著的离体抑制活性（抑制率51.7%⁸8.7%）.更多还原

【Abstract】 According to the drug design principle of active groups combination,a series of 5-( pyridine-3-yl)-1,2,4-triazole Mannich bases and bis-Mannich bases containing piperazine and fluorine moieties was designed and synthesized through the Mannich reaction of 1,2,4-triazole thiol intermediate. All the structures of new title compounds were characterized by ~1H NMR,13 C NMR and elemental analysis. The bioassay results showed that several compounds exhibited herbicidal activities against Brassica campestris in certain extent; compounds2 a,2d and 2f possessed significant antifungal activities against P. piricola and were comparable with the control fungicide,triadimefon,at the concentration of 50 mg / L. Also,compounds 2a,2b,2d and 2i showed favorable in vitro ketol-acid reductoisomerase( KARI) inhibitory activities with inhibition rate of 51. 7%—88. 7% at 180 mg / L.更多还原