摘要：

Flu or influenza remains a very serious respiratory illness. It is highly infective and causes periodic epidemics and pandemics. Protection against influenza through vaccination is limited due to the antigenic variation of the influenza virus, while the use of older antiviral agents amantadine and rimantadine is limited because of lack of activity against influenza B viruses, unfavorable tolerability and rapid emer- gence of resistance. Influenza neuraminidase inhibitors comprise a potent new compound class that was specifically designed to target the active site of the neuraminidase - sialidase enzyme, which is conserved across all type A and B influenza neuraminidase subtypes. The enzyme is essential for virus replication and infectivity. The successful strategy which has resulted in the development of potent influenza virus sialidase inhibitors relies on several factors: the information from the X-ray crystallographic studies of influenza virus sialidase; rational drug design tech- niques like molecular modelling and advances in computational chemistry analysis; and an understanding of the enzyme mechanism. Influenza neuraminidase has been validated as a target for the development of anti-influenza drugs as demonstrated by the efficiacy and selectivity of zanamivir and oseltamivir in the treatment and prevention of influenza virus infections.

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