Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-substituted dipyridodiazepinones as potent inhibitors of …

JR Proudfoot, KD Hargrave, SR Kapadia…

Index: Proudfoot; Hargrave; Kapadia; Patel; Grozinger; McNeil; Cullen; Cardozo; Tong; Kelly; Rose; David; Mauldin; Fuchs; Vitous; Hoermann; Klunder; Raghavan; Skiles; et al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 24 p. 4830 - 4838

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Citation Number: 45

Abstract

The major cause of viral resistance to the potent human immunodeficiency virus type 1 reverse transcriptase (RT) inhibitor nevirapine is the mutation substituting cysteine for tyrosine-181 in RT (Y181C RT). An evaluation, against Y181C RT, of previously described analogs of nevirapine revealed that the 2-chlorodipyridodiazepinone 16 is an effective inhibitor of this mutant enzyme. The detailed examination of the structure-activity ...