Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2. Tricyclic pyridobenzoxazepinones and dibenzoxazepinones

…, KD Hargrave, M West, E Cullen, K Pal…

Index: Klunder, Janice M.; Hargrave, Karl D.; West, MaryAnn; Cullen, Ernest; Pal, Kollol; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 10 p. 1887 - 1897

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Citation Number: 114

Abstract

Dibenz [b, fl [1, 4] oxazepin-ll (10H)-ones (111), pyrido [2, 3-b][1, 4] benzoxazepin-6 (5H)- ones (IV), and pyrido [2, 3-b]-[1, 5] benzoxazepin-5 (6H)-ones (V) were found to inhibit human immunodeficiency virus type 1 reverse transcriptase with ICm vduea as low as 19 nM. A-ring substitution has a profound effect on activity, with appropriate substituents at the positions ortho and para to the lactam nitrogen providing dramatically enhanced potency. ...