Author/Authors :
Paul G. Wyatt، نويسنده , , Barry A. Coomber، نويسنده , , Derek N. Evans، نويسنده , , Torquil I. Jack، نويسنده , , Heather E. Fulton، نويسنده , , Alan J. Wonacott، نويسنده , , Peter Colman، نويسنده , , Sudhir Kumar and Jose Varghese ، نويسنده ,
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.