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…

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

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被引用次数: 74

摘要

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 ...