NOVEL INHIBITORS OF INFLUENZA SIALIDASE RELATED TO GG167 - SYNTHESIS OF 4-AMINO AND GUANIDINO-4H-PYRAN-2-CARBOXYLIC ACID-6-PROPYLAMIDES - SELECTIVE INHIBITORS OF INFLUENZA-A VIRUS SIALIDASE

N-Propylcarboxamides 1a,b-3a,b have been synthesised from 3-didehydro- 2,4-dideoxy-4-amino-N-acetylneuraminic acid 4. The tertiary amides 2a, b-3a,b are highly potent but selective inhibitors of influenza A siali dase. The exceptional inhibitory activity of the dipropylamides 3a and 3b against influenza A shows that the 6-dipropylcarboxamide substitue nt is preferable to the polar glycerol sidechain found in the related sialidase inhibitors GG167 and 4. Copyright (C) 1996 Elsevier Science Ltd