Design, Synthesis, and in Vitro Biological Evaluation of 1H-1,2,3-Triazole-4-carboxamide Derivatives as New Anti-influenza A Agents Targeting Virus Nucleoprotein
Huimin Cheng
1, 2
,
Junting Wan
1
,
Meng-I Lin
3
,
Yingxue Liu
1
,
Xiaoyun Lu
1
,
Jinsong Liu
1
,
Yong Xu
1
,
Jianxin Chen
4
,
Zhengchao Tu
1
,
Yih-Shyun E. Cheng
3
,
Ke DING
1
Publication type: Journal Article
Publication date: 2012-02-27
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
22332894
Drug Discovery
Molecular Medicine
Abstract
The influenza virus nucleoprotein (NP) is an emerging target for anti-influenza drug development. Nucleozin (1) and its closely related derivatives had been identified as NP inhibitors displaying anti-influenza activity. Utilizing 1 as a lead molecule, we successfully designed and synthesized a series of 1H-1,2,3-triazole-4-carboxamide derivatives as new anti-influenza A agents. One of the most potent compounds, 3b, inhibited the replication of various H3N2 and H1N1 influenza A virus strains with IC(50) values ranging from 0.5 to 4.6 μM. Compound 3b also strongly inhibited the replication of H5N1 (RG14), amantidine-resistant A/WSN/33 (H1N1), and oseltamivir-resistant A/WSN/1933 (H1N1, 274Y) virus strains with IC(50) values in sub-μM ranges. Further computational studies and mechanism investigation suggested that 3b might directly target influenza virus A nucleoprotein to inhibit its nuclear accumulation.
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132
Total citations:
132
Citations from 2024:
15
(11.36%)
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GOST
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Cheng H. et al. Design, Synthesis, and in Vitro Biological Evaluation of 1H-1,2,3-Triazole-4-carboxamide Derivatives as New Anti-influenza A Agents Targeting Virus Nucleoprotein // Journal of Medicinal Chemistry. 2012. Vol. 55. No. 5. pp. 2144-2153.
GOST all authors (up to 50)
Copy
Cheng H., Wan J., Lin M., Liu Y., Lu X., Liu J., Xu Y., Chen J., Tu Z., Cheng Y. E., DING K. Design, Synthesis, and in Vitro Biological Evaluation of 1H-1,2,3-Triazole-4-carboxamide Derivatives as New Anti-influenza A Agents Targeting Virus Nucleoprotein // Journal of Medicinal Chemistry. 2012. Vol. 55. No. 5. pp. 2144-2153.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1021/jm2013503
UR - https://doi.org/10.1021/jm2013503
TI - Design, Synthesis, and in Vitro Biological Evaluation of 1H-1,2,3-Triazole-4-carboxamide Derivatives as New Anti-influenza A Agents Targeting Virus Nucleoprotein
T2 - Journal of Medicinal Chemistry
AU - Cheng, Huimin
AU - Wan, Junting
AU - Lin, Meng-I
AU - Liu, Yingxue
AU - Lu, Xiaoyun
AU - Liu, Jinsong
AU - Xu, Yong
AU - Chen, Jianxin
AU - Tu, Zhengchao
AU - Cheng, Yih-Shyun E.
AU - DING, Ke
PY - 2012
DA - 2012/02/27
PB - American Chemical Society (ACS)
SP - 2144-2153
IS - 5
VL - 55
PMID - 22332894
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2012_Cheng,
author = {Huimin Cheng and Junting Wan and Meng-I Lin and Yingxue Liu and Xiaoyun Lu and Jinsong Liu and Yong Xu and Jianxin Chen and Zhengchao Tu and Yih-Shyun E. Cheng and Ke DING},
title = {Design, Synthesis, and in Vitro Biological Evaluation of 1H-1,2,3-Triazole-4-carboxamide Derivatives as New Anti-influenza A Agents Targeting Virus Nucleoprotein},
journal = {Journal of Medicinal Chemistry},
year = {2012},
volume = {55},
publisher = {American Chemical Society (ACS)},
month = {feb},
url = {https://doi.org/10.1021/jm2013503},
number = {5},
pages = {2144--2153},
doi = {10.1021/jm2013503}
}
Cite this
MLA
Copy
Cheng, Huimin, et al. “Design, Synthesis, and in Vitro Biological Evaluation of 1H-1,2,3-Triazole-4-carboxamide Derivatives as New Anti-influenza A Agents Targeting Virus Nucleoprotein.” Journal of Medicinal Chemistry, vol. 55, no. 5, Feb. 2012, pp. 2144-2153. https://doi.org/10.1021/jm2013503.