Novel Non-Nucleoside Inhibitors of Human Immunodeficiency Virus Type 1 Reverse Transcriptase. 6. 2-Indol-3-yl-and 2-Azaindol-3-yl-dipyridodiazepinones 1

TA Kelly, DW McNeil, JM Rose, E David…

Index: Kelly; McNeil; Rose; David; Shih; Grob Journal of Medicinal Chemistry, 1997 , vol. 40, # 15 p. 2430 - 2433

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Citation Number: 74

Abstract

Nevirapine 2 (Viramune, 1) represents the first member of the non-nucleoside class of inhibitors of reverse transcriptase (RT) to receive approval for the treatment of human immunodeficiency virus (HIV) infections. This drug binds to an allosteric region on the protein and induces conformational changes that halt the polymerase activity of the enzyme. 3 In clinical settings, mutations to wild-type RT have been observed that are resistant to nevirapine and thus require that ...