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With the introduction of bioisosteres of the guanidinium group together with scaffold hopping, 35 zanamivir analogs with C-4-modification were synthesized, and their inhibitory activities against both group-1 and group-2 neuraminidase (H5N1 and H3N2) were determined. Compound D26 exerts the most potency, with IC(50) values of 0.58 and 2.72 μM against N2 and N1, respectively. Further preliminary anti-avian influenza virus (AIV, H5N1) activities against infected MDCK cells were evaluated, and D5 exerts ∼58% protective against AIV infection, which was comparable to zanamivir (∼67%). In a rat pharmacokinetic study, compound D5 showed an increased plasma half-life (t(1/2)) compared to zanamivir following either intravenous or oral administration. This study may represent a new start point for the future development of improved anti-AIV agents. Copyright © 2012 Elsevier Masson SAS. All rights reserved.


Deju Ye, Woo-Jin Shin, Ning Li, Wei Tang, Enguang Feng, Jian Li, Pei-Lan He, Jian-Ping Zuo, Hanjo Kim, Ky-Youb Nam, Weiliang Zhu, Baik-Lin Seong, Kyoung Tai No, Hualiang Jiang, Hong Liu. Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities. European journal of medicinal chemistry. 2012 Aug;54:764-70

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PMID: 22795831

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