Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities

Chien Hung Lin, Tsung Che Chang, Anindya Das, Ming Yu Fang, Hui Chen Hung, Kai Cheng Hsu, Jinn Moon Yang, Mark Von Itzstein, Kwok Kong T Mong, Tsu An Hsu, Chun Cheng Lin

研究成果: 雜誌貢獻文章

25 引文 斯高帕斯(Scopus)

摘要

A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative 3j, with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.
原文英語
頁(從 - 到)3943-3948
頁數6
期刊Organic and Biomolecular Chemistry
11
發行號24
DOIs
出版狀態已發佈 - 六月 28 2013
對外發佈Yes

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Biochemistry

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    Lin, C. H., Chang, T. C., Das, A., Fang, M. Y., Hung, H. C., Hsu, K. C., Yang, J. M., Von Itzstein, M., Mong, K. K. T., Hsu, T. A., & Lin, C. C. (2013). Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities. Organic and Biomolecular Chemistry, 11(24), 3943-3948. https://doi.org/10.1039/c3ob40624e