Rational Drug Design of Neuraminidase Inhibitors as Novel Anti-Influenza Agents

Influenza is a highly contagious infection of therespiratory tract and transmitted by droplets containinginfluenza viruses A, B or C. Spread of these pathogenicviral particles is responsible for the considerable globalpandemic disease. In the prophylaxis and treatment ofinfluenza, neuraminidase (NA), the enzyme cleaving aterminal sialic acid (SA) residue from glycoconjugatesenabling release of the virion from infected cells, hasbeen considered an ideal target for designing promisingtherapeutics. One of such potent and specific NAinhibitors is oseltamivir (Tamiflu®) which is a transitionstateanalog of SA derived from computer-aided rationaldrug design. Baicalein, a naturally-occurring polyphenolicconstituent of Scutellaria baicalensis Georgi and otherforage, has also been shown an important phytomedicineof interest as protectants against flu and other diseases.We report herein their design and relevant syntheticapproaches toward novel anti-influenza activities with NAas target.