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Ketones as Building Blocks for Dynamic Combinatorial Libraries:  Highly Active Neuraminidase Inhibitors Generated via Selection Pressure of the Biological Target

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posted on 03.01.2003, 00:00 authored by Matthias Hochgürtel, Ralf Biesinger, Heiko Kroth, Dorothea Piecha, Michael W. Hofmann, Sonja Krause, Otmar Schaaf, Claude Nicolau, Alexey V. Eliseev
New and potent inhibitors of neuraminidase, a key enzyme in the influenza virus activity, have been discovered in dynamic combinatorial libraries based on ketones and amines as building blocks. Selective synthesis of a number of inhibitors among multiple theoretically possible combinations of building blocks is driven by the presence of the target enzyme.