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Biology, Target Search and Drug Discovery

Organocatalytic approaches towards easy synthesized, economical and high yielding Tamiflu derivatives

EC contribution
: € 2.300.000,00
: 36 months
Starting date
: 01/04/2008
Funding scheme
: Collaborative Project - Small- or medium-scale focused research project
: influenza, tamiflu, neuraminidase inhibitors, influenza pandemic, Shikimic acid, oseltamivir phosphate, new drugs, organocatalysis
Contract/Grant agreement number
: 201431
Project web-site


Despite widespread immunization, influenza still kills thousand of people, and costs to the US, Europe and Asia enormous amounts of money in terms of healthcare expenses and productivity losses. While immunization remains an important approach to prevent influenza, small-molecule antiviral agents represent a novel opportunity for an effective prevention and therapy of flu. Inhibitors of neuraminidase (NA), essential enzyme for viral replication in all three classes of influenza viruses, has been recently found. Two of these inhibitors have reached the market, namely zanamivir and oseltamivir phosphate. The recent health concerns related to the avian flu have increased the demand for stockpiles of neuraminidase inhibitors, both as a reasonable frontline therapy against a possible flu pandemic and as a preventive agent. However, natural sources of Shikimic acid are scarce, and the increasing demand have put further pressure to develop new routes that do not involve complex natural products. In addition, there is the need to simplify the synthetic processes and make them less expensive in order to find new drug candidates, cut the drug costs and improve availability as well as efficiency, new chemical synthesis are necessary. The project proposes a new domino reaction based on an organocatalytic approach to the synthesis of new Tamiflu derivatives. The chemistry involved in this project is easy to perform, and can be well adapted to the industrial context. Moreover, new chemical structures will be prepared and evaluated as potential drug against virulent and mutated flu viruses.

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