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Novel inhibitors of influenza sialidases related to GG167 structure-activity, crystallographic and Molecular dynamics studies with 4H-pyran-2-carboxylic acid 6-carboxamides

✍ Scribed by Paul W. Smith; Steven L. Sollis; Peter D. Howes; Peter C. Cherry; Kevin N. Cobley; Helen Taylor; Andrew R. Whittington; Jan Scicinski; Richard C. Bethell; Neil Taylor; Tadeusz Skarzynski; Anne Cleasby; Oncar Singh; Alan Wonacott; Jose Varghese; Peter Colman

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 289 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(96)00542-2

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✦ Synopsis

The structure-activity relationships of a series of 4-amino and guanidino-4H-pyran-2carboxylic acid 6-carboxamides are described. These compounds represent a new class of inhibitor of influenza sialidases and are particularly active against influenza A sialidase. The binding of the Nphenethyl-N-propylamide 41 to influenza A and B sialidases has been investigated using X-ray crystallography and molecular dynamics simulations. Our results suggest that formation of a hitherto unobserved intramolecular salt bridge within the enzymes may account for the observed activity and selectivity of the series.

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