Chinese Journal of Organic Chemistry >
Synthesis and Biological Activities of Novel Pyrazole Amide Derivatives Containing Substituted Isoxazole Group
Received date: 2017-02-19
Revised date: 2017-03-09
Online published: 2017-04-01
Supported by
Project supported by the National Natural Science Foundation of China (No. 21372135), the Research Foundation of the Six People Peak of Jiangsu Province (No. 2013-SWYY-013), the Science and Technology Project Fund of Nantong City (No. MS22015020), and the Postgraduate Research and Practice Innovation Program of Jiangsu Province (No. SJCX17_0640).
In order to find novel pyrazole compounds possessing potent biological activities, a series of novel pyrazole amide derivatives bearing substituted isoxazole moiety were designed and synthesized according to the method of active substructure combination. Their structures were confirmed by 1H NMR, 13C NMR and elemental analysis. The bioassay data indicated that some title compounds had good insecticidal activities. At the concentration of 500 μg/mL, some compounds showed 60%~100% insecticidal activity against Oriental armyworm, and 50%~100% insecticidal activity against Aphis medicaginis. Additionally, some compounds exhibited good anti-cancer activity against HepG2 cells with the IC50 values of 14.2~18.9 μmol/L.
Key words： isoxazole; pyrazole; amide; synthesis; biological activity
Dai Hong , Yao Wei , Ye Linyu , Fang Yuan , Shi Yujun , Song Chan , Li Chunjian , Shi Jian . Synthesis and Biological Activities of Novel Pyrazole Amide Derivatives Containing Substituted Isoxazole Group[J]. Chinese Journal of Organic Chemistry, 2017 , 37(8) : 2165 -2171 . DOI: 10.6023/cjoc201702025
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