Concepedia

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

Chien‐Hung Lin, Tsung-Che Chang, Anindya Sundar Das, Mingyu Fang, Hui-Chen Hung, Kai‐Cheng Hsu, Jinn‐Moon Yang, Mark von Itzstein, Kwok Kong Tony Mong, Tsu-An Hsu,

Organic & Biomolecular Chemistry · 2013 · 32 citations · 27 references

DOI

Concepts

Abstract

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 , with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.

References

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