1. Academic Validation
  2. Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir)

Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir)

  • Bioorg Med Chem Lett. 2007 Sep 1;17(17):4851-4. doi: 10.1016/j.bmcl.2007.06.049.
Zong-Ying Liu 1 Bo Wang Li-Xun Zhao Yu-Huan Li Hua-Yi Shao Hong Yi Xue-Fu You Zhuo-Rong Li
Affiliations

Affiliation

  • 1 Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, China.
Abstract

Three alkoxyalkyl 2-carboxylate ester derivatives related to zanamivir were synthesized. All of the analogs of zanamivir modified at carboxylic moiety with alkoxyalkyl esters 1a-c showed higher activities than ribavirin on influenza A and B virus in the MDCK cells. Oral treatment or intraperitoneal administration of compound 1c showed significantly protective effects in mice infected with influenza A virus with low toxicities.

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