Discovery, synthesis, and bioactivity of bis (heteroaryl) piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors

…, RA Morge, C Biles, N Berrios-Pena…

文献索引：Romero; Morge; Biles; Berrios-Pena; May; Palmer; Johnson; Smith; Busso; Tan; Voorman; Reusser; Althaus; Downey; So; Resnick; Tarpley; Aristoff Journal of Medicinal Chemistry, 1994 , vol. 37, # 7 p. 999 - 1014

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被引用次数: 108

摘要

A variety of analogues of 1-[4-methoxy-3, 5-dimethylbenzyll-4-[3-(ethylamino)-2-pyridyl] piperazine hydrochloride (U-80493E) were synthesized and evaluated for their inhibition of human immunodeficiencyvirus type 1 (HIV-1) reverse transcriptase (RT). Replacement of the substituted aryl moiety with various substituted indoles provided bis (heteroary1) piperazines (BHAPs) that were l&lOO-fold more potent than U-80493E. The pyridyl portion ...