Citation: Chao Han, Yan-Chun Guo, Dan-Dan Wang, Xing-Jie Dai, Feng-Juan Wu, Huan-Fei Liu, Gui-Fu Dai, Jing-Chao Tao. Novel pyrazole fused heterocyclic ligands: Synthesis, characterization, DNA binding/cleavage activity and anti-BVDV activity[J]. Chinese Chemical Letters, ;2015, 26(5): 534-538. doi: 10.1016/j.cclet.2015.01.006 shu

Novel pyrazole fused heterocyclic ligands: Synthesis, characterization, DNA binding/cleavage activity and anti-BVDV activity

1.
a College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450052, China;
2.
b School of Life Sciences, Zhengzhou University, Zhengzhou 450001, China

Corresponding author: Gui-Fu Dai, Jing-Chao Tao,
Received Date: 6 November 2014
Available Online: 12 December 2014
Fund Project:

A series of novel pyrazole fused heterocyclic derivatives were synthesized via a two-step procedure or a one-pot two step method, and their catalytic DNA cleavage abilities and anti-BVDV activities were also evaluated. The results obtained indicated that compounds 3b-3c could catalyze the cleavage of supercoiled DNA (pUC 19 plasmid DNA) to nicked DNA under physiological conditions with high yields via a hydrolytic mechanism. The studies on anti-viral activities against bovine viral diarrhea virus (BVDV) demonstrated that some of the pyrazole derivatives showed pronounced anti-BVDV activity with interesting EC5₀ values and no significant cytotoxicity. Among them, compound 3l showed the highest antiviral activity (EC5₀ = 0.12 μmol/L) and was 10 fold more than that of the positive control ribavirin (EC5₀ = 1.3 μmol/L), which provided a potential candidate for the development of anti-BVDV agents.
- Synthesis,
- Tetramic acids,
- DNA binding/cleavage,
- Pyrazole derivatives,
- Anti-BVDV
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1.
沈阳化工大学材料科学与工程学院沈阳 110142