Anti-influenza agents

Madren LK, Shipman C, Hayden FG. In vitro inhibitory effects of combinations of anti-influenza agents. Antiviral Chem Chemotherapy 1995 6(2) 109—113. 

The new anti-influenza agent, LY217896, 86, active against both A and B strains of influenza75, has been 14C and 13C labelled76 to support the pre-clinical as well as clinical drug 86 metabolism and disposition studies and to facilitate the identification of metabolism of 86 in vivo. 

Shie J-J, Fang J-M, Wong C-H (2008) A Concise and Flexible Synthesis of the Potent Anti-Influenza Agents Tamiflu and Tamiphosphor. Angew Chem Int Ed 47 5788... 

Because of the essential role of sialidase in influenza virus replication and the highly conserved enzyme active-site in influenza viruses A and B, most interest has been focused on the development of selective inhibitors of this enzyme.10 This chapter discusses the tremendous progress that has been made in the discovery of this new class of anti-influenza agents, in addition to some background information to understand the fundamental role of influenza. 

J. Zhang and W. Xu, Recent advances in anti-influenza agents with neuraminidase as target, Mini Rev. Med. Chem., 6 (2006) 429-448. 

Matveenko M, Willis AC et al (2008) A chemoenzymatic synthesis of the anti-influenza agent Tamiflu . Tetrahedron Lett 49 7018-7020... 

DESIGN AND SYNTHESIS OF CARBOHYDRATES AND CARBOHYDRATE MIMETICS AS ANTI-INFLUENZA AGENTS... 

After these surface interactions have taken place and the virus has been taken into the cell, another viral protein, neuramidase, cleaves the glycosidic bonds to the sialic acid residues, freeing the virus to infect the cell. Inhibitors of this enzyme are showing some promise as anti-influenza agents. 

Mineno, T., Miller, M. J. Stereoselective Total Synthesis of Racemic BCX-1812 (RWJ-270201) for the Development of Neuraminidase Inhibitors as Anti-influenza Agents. J. Org. Chem. 2003, 68, 6591-6596. 

Several excellent articles describing various aspects of influenza virus, both with respect to the virus itself as well as approaches towards the development of anti-influenza agents, have been published in recent years [4-16]. In view of the comprehensive nature of these reports it is the aim of this account, apart from providing the background information necessary to a fundamental understanding of influenza, to focus on advances in the development of influenza virus sialidase inhibitors over the last decade. ... 

Since haemagglutinin is involved in the adhesion of influenza virus to epithelial cells, it is an attractive target for therapeutic intervention. The design and synthesis of potential inhibitors of haemagglutinin has been reviewed elsewhere [5, 7, 14, 17, 33, 34] and, apart from a brief discussion of the general approaches employed towards such anti-influenza agents, is outside the scope of this article. 

The products are useful building blocks for the synthesis of more complex molecules. Both the diastereos-elective and the enantioselective reactions were combined in a synthesis of fluviricin Bi 5.288, an antifungal and anti-influenza agent (Scheme 5.78). Of the two fragments required for the formation of the macrocycle. 

RWJ-270201), a neuramidase inhibitor used as an anti-influenza agent. ... 

A synthetic approach to the anti-influenza agent, A-215675 (143) made use of an embedded Weinreb amide. The chiral aldehyde 141 was treated with functionalized ylide generated from 140 to afford 142. The Weinreb amide moiety was then used to elaborate 142 to the desired target 143. 

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