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Approaches to carbocyclic sialidase inhibitors

By Hans Streicher


The crucial role played by carbohydrates in many physiological processes has made this class of compounds an interesting target for drug design. Consequently mimicking carbohydrates has been one of the most rapidly growing fields in synthetic organic chemistry in recent years, and particularly intense focus has been devoted to sialic acids and sialic acid metabolizing enzymes, including sialidases. Inhibition of the latter enzyme from influenza virus can be regarded as one of the most successful examples of structure-based drug design and high affinity inhibitors based on neuraminic acid have been developed. There is an ongoing search for inhibitors with improved physicochemical properties and among them, carbocyclic systems, where the ring oxygen of the carbohydrate is replaced by carbon, have become the center of interest. This review intends to give a brief overview over the structures and synthetic approaches which surfaced in the last decade

Publisher: Springer Verlag
Year: 2002
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