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.
ASJC Scopus subject areas
- Physical and Theoretical Chemistry
- Organic Chemistry
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