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

作　　者：KANG Yan-fang WANG Dun-jia XU Ben-po WEI Xian-hong ZHENG Jing 

机构地区：[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

出　　处：《Chemical Research in Chinese Universities》2013年第2期227-230,共4页高等学校化学研究（英文版）

基　　金：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）, IH NMR, mass spectroscopy and elemental analysis. The biological activities of the title compounds were examined by disc diffusion method against Escherichia coil 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.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）, IH NMR, mass spectroscopy and elemental analysis. The biological activities of the title compounds were examined by disc diffusion method against Escherichia coil 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 fl-Diketone 1H-Pyrazole Biological activity 

分 类 号：O626.21[理学—有机化学] S482.39[理学—化学]