Beilstein J. Org. Chem.2009,5, No. 36, doi:10.3762/bjoc.5.36
, Ubonratchathani 34190, Thailand 10.3762/bjoc.5.36 Abstract Ten dipyridodiazepinone derivatives were synthesized and evaluated for their anti HIV-1 reverse transcriptase activity against wild-type and mutant type enzymes, K103N and Y181C. Two of them were found to be promising inhibitors for HIV-1 RT.
Keywords
: AIDS; anti HIV-1 RT; dipyridodiazepinone; nevirapine; synthesis; Introduction
Dipyridodiazepinone nevirapine (1) [1] (Figure 1) is a potent non-nucleoside inhibitor of human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) and is approved as a therapeutic agent for the treatment of AIDS
. In the clinic, nevirapine monotherapy results in relatively rapid drug resistance due to mutation of the RT enzyme. To develop a second-generation inhibitor with improved activity against the mutant RT enzyme, many efforts have been focused on the synthesis of dipyridodiazepinone derivatives [2][3][4