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Molecules 2013, 18(4), 3789-3805; doi:10.3390/molecules18043789

Synthesis and Anti-Influenza Virus Activities of a Novel Class of Gastrodin Derivatives

, , , , , , , , * ,  and *
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
* Authors to whom correspondence should be addressed.
Received: 16 February 2013 / Revised: 19 March 2013 / Accepted: 20 March 2013 / Published: 26 March 2013
(This article belongs to the Section Medicinal Chemistry)
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A series of substituted aryl glycoside analogues of gastrodin have been identified as potential anti-influenza agents. The most potent inhibitor 1a exhibited moderate inhibitory activity against the A/Hanfang/359/95(H3N2) and A/FM/1/47(H1N1) strains of the influenza A virus (IC50 values of 44.40 and 34.45 μM, respectively) and the oseltamivir-null B/Jifang/13/97 strain of influenza B (IC50 value of 33.01 μM). In this article, multiple doses of compound 1a (80 mg/kg/day, oral administration) were used for the treatment of mice infected with influenza A/FM/1/47-MA (H1N1), and surprisingly we found that compound 1a significantly increased the number of survivors and prolonged the mean survival time. The preliminary studies on the mechanism of antiviral activity showed no interaction between compound 1a and the neuraminidase or the M2 protein. The novel target to overcome drug resistance combined with its good in vivo profile support compound 1a to be a new lead for further development of antiviral agents.
Keywords: gastrodin; aryl glycoside; synthesis; influenza virus inhibitors gastrodin; aryl glycoside; synthesis; influenza virus inhibitors
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Xue, S.-T.; He, W.-Y.; Ma, L.-L.; Wang, H.-Q.; Wang, B.; Zheng, G.-H.; Ji, X.-Y.; Zhang, T.; Li, Y.-H.; Jiang, J.-D.; Li, Z.-R. Synthesis and Anti-Influenza Virus Activities of a Novel Class of Gastrodin Derivatives. Molecules 2013, 18, 3789-3805.

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