Haemagglutinin-based inhibitors

Scheme 4.13. Dendritic sialoside inhibitors of influenza A virus haemagglutinin constructed via the solid phase synthesis of a lysine-based superstructure.

Influenza vims A has two surface glycoproteins that offer potential for the development of competitive multivalent sugar clusters featuring 5-A -acetyl neuraminic acid (Neu5Ac) units [35]. Haemagglutinin (HA) binds to sialic acid receptors and fuses the cell membranes of the vims and host and neuraminidase (NA), an enzyme, cleaves sialic acid residues and is involved in release of new vims by the host cell. Whilst small molecule inhibitors of NA, such as oseltamivir (Tamiflu) and zanamavir (Relenza), are now available, no therapy based on inhibition of binding of HA has reached the clinic. 

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