Synthesis,Crystal Structure and Anti-fungal/Anti-oomycete Activity of New Pyrazole-benzene Carboxamide Derivatives

• 作者: YANG Zi-Hui LIU Qing-Song SUN Yue SUN Xue-Bao GU Wen
• 来源期刊: 结构化学
• 年，卷（期）: 2022,（3）
• 页码范围: 253-259
• 页数: 7页
• 语种: 英文
• DOI: 10.14102/j.cnki.0254-5861.2011-3360

摘要

Four novel pyrazole-benzene carboxamide derivatives 2a～2d were synthesized and character-ized by NMR,HRMS spectral method and X-ray diffraction analysis,and were further conducted for screening the anti-fungal/anti-oomycete activity.Compound 2d crystallizes as monoclinic space group P21/c with a=42.260(4),b=5.3751(4),c=8.0129(9)?,β=92.958(10)°,V=1817.7(3)?3,Z=4,Mr=385.41,Dc=1.408 Mg/m3,S=1.087,μ=0.773 mrr-1,F(000)=808,the final R=0.0763 and wR=0.2136 for 2657 observed reflec-tions(I＞2σ(I)).The preliminary antifungal assay indicates that the title compounds show fair to excellent anti-fungal/anti-oomycete activity toward four plant fungi and two crop oomycetes.Among them,compound 2b ex-hibits the strongest in vitro anti-B.cinerea effects(EC50=1.61 mg/L).In vivo test presents compound 2b displays considerable protective and curative effects to tomato fruits infected by B.cinerea.These results indicate that compound 2b would be potential fungicides leads for further development.