title: Influenza Neuraminidase Inhibitors: Synthetic Approaches, Derivatives and Biological Activity.
abstract: Despite being a common viral disease, influenza has very negative consequences, causing the death of around half a million people each year. A neuraminidase located on the surface of the virus plays an important role in viral reproduction by contributing to the release of viruses from infected host cells. The treatment of influenza is mainly based on the administration of neuraminidase inhibitors. The neuraminidase inhibitors zanamivir, laninamivir, oseltamivir and peramivir have been commercialized and have been demonstrated to be potent influenza viral neuraminidase inhibitors against most influenza strains. In order to create more potent neuraminidase inhibitors and fight against the surge in resistance resulting from naturally-occurring mutations, these anti-influenza drugs have been used as templates for the development of new neuraminidase inhibitors through structure-activity relationship studies. Here, we review the synthetic routes to these commercial drugs, the modifications which have been performed on these structures and the effects of these modifications on their inhibitory activity.
authors.affiliation: Glycomics and Glycan Bioengineering Research Center, College of Food Science and Technology, Nanjing Agricultural University, 1 Weigang, Nanjing 210095, China. pedro.laborda@njau.edu.cn.
authors.forename: Pedro
authors.initials: P
authors.lastname: Laborda
authors.affiliation: Glycomics and Glycan Bioengineering Research Center, College of Food Science and Technology, Nanjing Agricultural University, 1 Weigang, Nanjing 210095, China. wangsuyan1008@126.com.
authors.forename: Su-Yan
authors.initials: SY
authors.lastname: Wang
authors.affiliation: Glycomics and Glycan Bioengineering Research Center, College of Food Science and Technology, Nanjing Agricultural University, 1 Weigang, Nanjing 210095, China. josef.voglmeir@njau.edu.cn.
authors.forename: Josef
authors.initials: J
authors.lastname: Voglmeir
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D006801:Humans; D007251:Influenza, Human / Q000188:drug therapy; D009439:Neuraminidase / Q000037:antagonists & inhibitors*; D009975:Orthomyxoviridae / Q000187:drug effects* / Q000201:enzymology*; D014764:Viral Proteins / Q000037:antagonists & inhibitors*
chemical_list: D000998:Antiviral Agents; D014764:Viral Proteins; D009439:Neuraminidase
keywords: influenza treatment; neuraminidase inhibitors; organic synthesis; sialic acid analogues; total synthesis