Hw. Hamilton et al., 6-PHENYL-6-ALKYLAMIDO-5,6-DIHYDRO-2H-PYRAN-2-ONES - NOVEL HIV PROTEASE INHIBITORS, Bioorganic & medicinal chemistry letters, 6(6), 1996, pp. 719-724
Publications from our laboratories have recently described a series of
3-thioaryl substituted-4-hydroxy-pyrones(1) as HIV protease inhibitor
s. The current work examines the analogous 5,6-dihydro-2H-pyran-2-ones
with 6,6-substitutions focusing on the use of 1 degrees, 2 degrees, a
nd 3 degrees alkyl amides of various chain lengths to fill the S1 thro
ugh S3 enzyme pockets.