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

tetano

Editor, Senior Moderator
Org Biomol Chem. 2013 May 22. [Epub ahead of print]
Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities.
Lin CH, Chang TC, Das A, Fang MY, Hung HC, Hsu KC, Yang JM, von Itzstein M, Mong KK, Hsu TA, Lin CC.
Source

Department of Chemistry, National Tsing Hua University, 101, Section 2, Kuang-Fu Road, Hsinchu 30013, Taiwan.
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.

PMID:
23695381
[PubMed - as supplied by publisher]

http://www.ncbi.nlm.nih.gov/pubmed/23695381
 
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