The Research Institute of Elemento-Organic Chemistry, State-Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin, China.
Chem Biol Drug Des. 2011 Jul;78(1):42-9. doi: 10.1111/j.1747-0285.2011.01132.x. Epub 2011 May 31.
A series of novel Mannich bases with trifluoromethyl-1,2,4-triazole and substituted benzylpiperazine moieties were synthesized. Their structures were confirmed by IR, (1) H NMR and elemental analysis. The single crystal structure of compound 4r was also determined. The preliminary bioassays showed that most of the lead compounds had low herbicidal activity against Brassica campestris, Echinochloa crusgalli, and KARI enzyme. However, most of them exhibited significant fungicidal activity at the dosage of 50 μg/mL toward five test fungi. Among the 18 novel compounds, several showed superiority over the commercial fungicide Triadimefon against Cercospora arachidicola and Fusarium oxysporum f. sp. cucumerinum during this study. Meanwhile, some compounds displayed plant growth regulatory activity at the dosage of 10 μg/mL.
一系列含有三氟甲基-1,2,4-三唑和取代苄基哌嗪部分的新型曼尼希碱被合成。它们的结构通过 IR、(1)H NMR 和元素分析得到确认。化合物 4r 的单晶结构也被确定。初步的生物测定表明，大多数先导化合物对油菜、稗草和 KARI 酶表现出低除草活性。然而，在 50 μg/mL 的剂量下，它们对五种测试真菌均表现出显著的杀菌活性。在这 18 种新型化合物中，有几种在研究中对花生褐斑病菌和黄瓜枯萎病菌表现出优于商业杀菌剂三唑酮的优势。同时，一些化合物在 10 μg/mL 的剂量下显示出植物生长调节活性。
