A series of unique 3,3a-dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones and a
2a,5-dihydro-2H-thieno[4,3,2-de]quinazoline-4(3H)-thione were found to be H
IV-1 non-nucleoside reverse transcriptase inhibitors. One of these compound
s, as the racemate, possessed an IC90 = 4.6 nM against wild-type virus in a
whole cell antiviral assay and had an IC90 = 76 and 897 nM against the cli
nically significant K103N and K103N/L100I mutant viruses, respectively. (C)
2001 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. Al
l rights reserved.