Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides |
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| Authors: | Wyatt P G Coomber B A Evans D N Jack T I Fulton H E Wonacott A J Colman P Varghese J |
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| Institution: | Department of Medicinal Chemistry, Glaxo Wellcome Medicines Research Centre, Stevenage, Herts, UK. pw29967@glaxowellcome.co.uk |
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| Abstract: | SAR investigations of the 4- and 5-positions of a series of 4-amino-4H-pyran-2-carboxylic acid 6-carboxamides are reported. Potent inhibitors of influenza A sialidase with marked selectivity over the influenza B enzyme were obtained when the basic 4-amino substituent was replaced by hydroxyl or even deleted. Modifications at the 5-position exhibited a tight steric requirement, with trifluoroacetamide being optimal. |
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