ChemInform Abstract: Sialidase Inhibitors Related to Zanamivir. Further SAR Studies of 4-Amino-4H-pyran-2-carboxylic Acid-6-propylamides

Autor:	Heather E. Fulton, Torquil I. Jack, Derek N. Evans, Barry A. Coomber, Peter M. Colman, Paul Wyatt, Jose Varghese, Alan J. Wonacott
Rok vydání:	2010
Předmět:	chemistry.chemical_classification Steric effects Stereochemistry Carboxylic acid Substituent General Medicine Sialidase chemistry.chemical_compound Enzyme Zanamivir chemistry Pyran medicine Selectivity medicine.drug
Zdroj:	ChemInform. 32
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200122144
Popis:	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.
Databáze:	OpenAIRE
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