新型含取代哌嗪的5-(吡啶-3-基)-1,2,4-三唑Mannich碱和双Mannich碱的合成及生物活性
摘要
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 H-1 NMR, C-13 NMR and elemental analysis. The bioassay results showed that several compounds exhibited herbicidal activities against Brassica campestris in certain extent; compounds 2a, 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.