Design, synthesis and anti-tobacco mosaic virus (TMV) activity of 5-chloro-N-(4-cyano-1-aryl-1H-pyrazol-5-yl)-1-aryl-3-methyl-1H-pyrazole-4-carboxamide derivatives.
Design, synthesis and anti-tobacco mosaic virus (TMV) activity of 5-chloro-N-(4-cyano-1-aryl-1H-pyrazol-5-yl)-1-aryl-3-methyl-1H-pyrazole-4-carboxamide derivatives.
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DOI：
10.3390/molecules20010807
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发表时间：
2015-01-07
期刊：
影响因子：
--
通讯作者：
Cao HQ
中科院分区：
文献类型：
--
作者：
Xiao JJ;Liao M;Chu MJ;Ren ZL;Zhang X;Lv XH;Cao HQ
以5-氯-1-芳基-3-甲基-1H-吡唑-4-羧酸和5-氨基-1-芳基-1H-吡唑-4-腈为原料，设计合成了一系列以烟草花叶病毒PC蛋白为靶标的新型吡唑酰胺衍生物3a-3 p。所有化合物均通过1H-NMR、质谱和元素分析进行了表征。初步生物活性测定结果表明，在500 μg/mL浓度下，所有化合物均表现出较好的抗烟草花叶病毒（TMV）活性。其中化合物3 p对烟草花叶病毒（TMV）的生物活性最强，结合模型表明吡唑酰胺部分紧密嵌入TMV PC（PDB代码：2 OM 3）的结合位点。
A series of novel pyrazole amide derivatives 3a–3p which take TMV PC protein as the target has been designed and synthesized by the reactions of 5-chloro-1-aryl-3-methyl-1H-pyrazole-4-carboxylic acids with 5-amino-1-aryl-1H-pyrazole-4-carbonitriles. All the compounds were characterized by 1H-NMR, mass spectroscopy and elemental analysis. Preliminary bioassays indicated that all the compounds acted against the tobacco mosaic virus (TMV) with different in vivo and in vitro modes at 500 μg/mL and were found to possess promising activity. Especially, compound 3p showed the most potent biological activity against tobacco mosaic virus (TMV) compared to ningnanmycin, and a molecular docking study was performed and the binding model revealed that the pyrazole amide moiety was tightly embedded in the binding sites of TMV PC (PDB code: 2OM3).
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影响因子：
7.3
作者：
Fleming FF;Yao L;Ravikumar PC;Funk L;Shook BC
通讯作者：
Shook BC
影响因子：
6.7
作者：
Rida, SM;Ashour, FA;Shalaby, MA
通讯作者：
Shalaby, MA
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6.1
作者：
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影响因子：
1.5
作者：
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通讯作者：
Brovarets, V. S.
影响因子：
4.1
作者：
Siddall, TL;Ouse, DG;Weimer, MR
通讯作者：
Weimer, MR