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高等学校化学研究 ›› 2013, Vol. 29 ›› Issue (2): 227-230.doi: 10.1007/s40242-013-2469-0

• Articles • 上一篇    下一篇

Synthesis, Characterization and Biological Activities of N-Acyl-3-(3-pyridyl)-5-aryl-pyrazoles

KANG Yan-fang, WANG Dun-jia, XU Ben-po, WEI Xian-hong, ZHENG Jing   

  1. Hubei Provincial Key Laboratory of Pollutant Analysis and Reuse Technology, College of Chemistry and Environmental Engineering, Hubei Normal University, Huangshi 435002, P. R. China
  • 收稿日期:2012-12-04 修回日期:2012-12-27 出版日期:2013-04-01 发布日期:2013-03-20
  • 通讯作者: WANG Dun-jia E-mail:dunjiawang@163.com
  • 基金资助:

    Supported by the National Natural Science Foundation of China(No.21273065).

Synthesis, Characterization and Biological Activities ofN-Acyl-3-(3-pyridyl)-5-aryl-pyrazoles

KANG Yan-fang, WANG Dun-jia, XU Ben-po, WEI Xian-hong, ZHENG Jing   

  1. Hubei Provincial Key Laboratory of Pollutant Analysis and Reuse Technology, College of Chemistry and Environmental Engineering, Hubei Normal University, Huangshi 435002, P. R. China
  • Received:2012-12-04 Revised:2012-12-27 Online:2013-04-01 Published:2013-03-20
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.21273065).

摘要:

Ten novel N-acyl-3-(3-pyridyl)-5-aryl-pyrazoles were synthesized by Claisen condensation of the aryl methyl ketones with ethyl nicotinate, the cyclization with hydrazine hydrate and the N-acylation with acyl chloride in turn. The structures of all the compounds synthesized were confirmed by means of Fourier transform infrared(FTIR), 1H NMR, mass spectroscopy and elemental analysis. The biological activities of the title compounds were examined by disc diffusion method against Escherichia coli, Staphylococcus aureus, Pyricularia oryzae and Rhizoctnia solani. All the N-acyl-3-(3-pyridyl)-5-aryl-pyrazoles exhibited a certain degree of antibacterial and antifungal activities. Comparatively, compounds 3c and 3d exhibited much significant antibacterial and antifungal activities than the other pyrazole derivatives.

关键词: N-Acyl-3-(3-pyridyl)-5-aryl-pyrazole, b-Diketone, 1H-Pyrazole, Biological activity

Abstract:

Ten novel N-acyl-3-(3-pyridyl)-5-aryl-pyrazoles were synthesized by Claisen condensation of the aryl methyl ketones with ethyl nicotinate, the cyclization with hydrazine hydrate and the N-acylation with acyl chloride in turn. The structures of all the compounds synthesized were confirmed by means of Fourier transform infrared(FTIR), 1H NMR, mass spectroscopy and elemental analysis. The biological activities of the title compounds were examined by disc diffusion method against Escherichia coli, Staphylococcus aureus, Pyricularia oryzae and Rhizoctnia solani. All the N-acyl-3-(3-pyridyl)-5-aryl-pyrazoles exhibited a certain degree of antibacterial and antifungal activities. Comparatively, compounds 3c and 3d exhibited much significant antibacterial and antifungal activities than the other pyrazole derivatives.

Key words: N-Acyl-3-(3-pyridyl)-5-aryl-pyrazole, b-Diketone, 1H-Pyrazole, Biological activity