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Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities
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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, …
Organic and Biomolecular Chemistry, 卷.11(24), 頁碼.3943-3948
06/2013
DOI: https://doi.org/10.1039/c3ob40624e

摘要

Biochemistry Physical and Theoretical Chemistry Organic Chemistry
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. © The Royal Society of Chemistry 2013.

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