新型含取代吡唑基或 1,2,3-三唑基部分的氰基丙烯酸酯化合物的设计、合成及生物活性。
Design, Synthesis, and Biological Activities of Novel 2-Cyanoacrylate Compounds Containing Substituted Pyrazolyl or 1,2,3-Triazolyl Moiety.
机构信息
College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, China.
出版信息
Molecules. 2023 Mar 31;28(7):3141. doi: 10.3390/molecules28073141.
To develop novel 2-cyanoacrylate derivatives with potential bioactivity, a number of 2-cyanoacrylate compounds, including substituted pyrazole or 1,2,3-triazole ring, were designed, prepared, and structurally detected by H NMR, C NMR, and elemental analysis. The biological assessment displayed that some designed compounds had significant herbicidal activities against , , , , and at a dosage of 1500 g/ha. Furthermore, some derivatives still expressed satisfactory herbicidal activities against , and when the dosage was lowered to 150 g/ha, especially the inhibitory effects of compounds , , , , , , , and against were all over 80%, compounds , , , , , , , , , and possessed more than 70% inhibition rates against , and compound indicated 70% herbicidal activity against . These results provided an important basis for further design and discovery of biologically active 2-cyanoacrylate compounds.
为了开发具有潜在生物活性的新型 2-氰基丙烯酸酯衍生物，设计、合成了一系列取代吡唑或 1,2,3-三唑环的 2-氰基丙烯酸酯化合物，并通过 1H NMR、13C NMR 和元素分析进行了结构确证。生物评价结果表明，部分设计的化合物在 1500 g/ha 的剂量下对稗草、马唐、狗尾草、反枝苋、马齿苋和苘麻具有显著的除草活性。此外，当剂量降低至 150 g/ha 时，部分衍生物对鸭跖草、藜和龙葵仍表现出良好的除草活性，特别是化合物 、 、 、 、 、 、 对稗草的抑制率均在 80%以上，化合物 、 、 、 、 、 、 、 对马唐的抑制率均在 70%以上，化合物 对反枝苋的抑制率为 70%。这些结果为进一步设计和发现具有生物活性的 2-氰基丙烯酸酯化合物提供了重要依据。
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