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

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

Le Tao ¹, Yujiang Li ¹, Xiaohe Guo ², Lihong Dong ¹, Luping Liu ¹, Qiang Wang ¹, Xuejun Yu ¹, Chuanjun Song ³, Junbiao Chang ⁴

Affiliations

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: [email protected].
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: [email protected].

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

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.

Name
Email *

	Sorry, but the email address you supplied was invalid.