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

被引：34

作者：

Lin, Chien-Hung ^{[1
]}

Chang, Tsung-Che ^{[1
]}

Das, Anindya ^{[1
]}

Fang, Ming-Yu ^{[2
]}

Hung, Hui-Chen ^{[2
]}

Hsu, Kai-Cheng ^{[3
,4
]}

Yang, Jinn-Moon ^{[3
,4
]}

von Itzstein, Mark ^{[5
]}

Mong, Kwok Kong T. ^{[3
,4
]}

Hsu, Tsu-An ^{[2
]}

Lin, Chun-Cheng ^{[1
]}

机构：

[1] Natl Tsing Hua Univ, Dept Chem, Hsinchu 30013, Taiwan

[2] Natl Hlth Res Inst, Div Biotechnol & Pharmaceut Res, Zhunan 35053, Taiwan

[3] Natl Chiao Tung Univ, Dept Biol Sci & Technol, Hsinchu 30010, Taiwan

[4] Natl Chiao Tung Univ, Dept Appl Chem, Hsinchu 30010, Taiwan

[5] Griffith Univ, Inst Glyc, Southport, Qld 4222, Australia

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2013年 / 11卷 / 24期

关键词：

INFLUENZA-A VIRUS; ANALOGS; DESIGN; ACID; CONFORMATIONS; OSELTAMIVIR; BINDING; PHASE;

D O I：

10.1039/c3ob40624e

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：3943 / 3948

页数：6

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