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Bioorg Med Chem Lett. 2020 Jan 1;30(1):126770. doi: 10.1016/j.bmcl.2019.126770. Epub 2019 Oct 28.

Synthesis and anti-CVB3 activity of 4-amino acid derivative substituted pyrimidine nucleoside analogues.

Author information

1
High & New Technology Research Center of Henan Academy of Sciences, Zhengzhou, Henan Province 450002, PR China.
2
High & New Technology Research Center of Henan Academy of Sciences, Zhengzhou, Henan Province 450002, PR China. Electronic address: zhangshengqian@ncwu.edu.cn.
3
College of Chemistry, Zhengzhou University, Zhengzhou, Henan Province 450001, PR China.
4
Henan Key Laboratory of Organic Functional Molecules and Drug Innovation, Henan Normal University, Xinxiang 453007, PR China. Electronic address: cjb@htu.edu.cn.

Abstract

Seven novel 4-amino acid derivative substituted pyrimidine nucleoside analogues were designed, synthesized, and tested for their anti-CVB3 activity. Initial biological studies indicated that among these 4-amino acid derivative substituted pyrimidine nucleoside analogues, 4-N-(2'-amino-glutaric acid-1'-methylester)-1-(2'- deoxy-2'-β-fluoro-4'-azido)-furanosyl-cytosine 2 exhibited the most potent anti-CVB activity (IC50 = 9.3 μM). The cytotoxicity of these compounds has also been assessed. The toxicity of compound 2 was similar to that of ribavirin.

KEYWORDS:

Amino acid; Anti-CVB3 activity; Pyrimidine nucleoside; Synthesis

PMID:
31735601
DOI:
10.1016/j.bmcl.2019.126770

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