Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo-and dipyridodiazepinones

KD Hargrave, JR Proudfoot, KG Grozinger…

Index: Hargrave, Karl D.; Proudfoot, John R.; Grozinger, Karl G.; Cullen, Ernest; Kapadia, Suresh R.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 7 p. 2231 - 2241

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Citation Number: 215

Abstract

Novel pyrido [2, 3-b][1, 4] benzodiazepinones (I), pyrido [2, 3-b][1, 5] benzodiazepinones (II), and dipyrido [3, 2-b: 2', 3'-e][1, 4] diazepinones (111) were found to inhibit human immunodeficiency virus type 1 (HIV-1) reverse transcriptase in vitro at concentrations as low as 35 nM. In all three series, small substituents (eg, methyl, ethyl, acetyl) are preferred at the lactam nitrogen, whereas slightly larger alkyl moieties (eg, ethyl, cyclopropyl) are favored ...