Novel 3,4-disubstituted-Neu5Ac2en derivatives as probes to investigate flexibility of the influenza virus sialidase 150-loop |
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Authors: | Santosh Rudrawar Jeffrey C Dyason Andrea Maggioni Robin J Thomson Mark von Itzstein |
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Institution: | 1. University of Oxford, Dept. of Chemistry, Mansfield Road, Oxford, OX1 3TA, UK |
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Abstract: | Novel 3,4-disubstituted-Neu5Ac2en derivatives have been synthesised to probe the open 150-loop conformation of influenza virus sialidases. Both equatorially and axially (epi) substituted C4 amino and guanidino 3-(p-tolyl)allyl-Neu5Ac2en derivatives were prepared, via the 4-epi-hydroxy derivative. The equatorially-substituted 4-amino derivative showed low micromolar inhibition of both group-1 (pdm09 H1N1) and group-2 (pdm57 H2N2) sialidases, and provides the first in vitro evidence that a group-2 sialidase may exhibit 150-loop flexibility. |
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Keywords: | Influenza Sialidase 150-loop Neu5Ac2en Sialic acid |
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