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3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors
J W Corbett1, S Pan, J A Markwalder
1DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA. jeffrey.w.corbett@am.pnu.com
Bioorganic & Medicinal Chemistry Letters
|February 24, 2001
Abstract:
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]quinazo-line-4(3H)-thione were found to be HIV-1 non-nucleoside reverse transcriptase inhibitors. One of these compounds, 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 clinically significant K103N and K103N/L100I mutant viruses, respectively.