Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides

TY - JOUR

T1 - Sialidase inhibitors related to zanamivir. Further SAR studies of 4-amino-4H-pyran-2-carboxylic acid-6-propylamides

AU - Wyatt, Paul G.

AU - Coomber, Barry A.

AU - Evans, Derek N.

AU - Jack, Torquil I.

AU - Fulton, Heather E.

AU - Wonacott, Alan J.

AU - Colman, Peter

AU - Varghese, Jose

N1 - dc.publisher: Elsevier

PY - 2001/3

Y1 - 2001/3

N2 - 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.

AB - 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.

U2 - 10.1016/S0960-894X(01)00019-1

DO - 10.1016/S0960-894X(01)00019-1

M3 - Article

SN - 0960-894X

VL - 11

SP - 669

EP - 673

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 5

ER -