Design, synthesis, and biological activity of novel 1, 4-disubstituted piperidine/piperazine derivatives as CCR5 antagonist-based HIV-1 entry inhibitors

M Dong, L Lu, H Li, X Wang, H Lu, S Jiang…

文献索引：Dong, Ming-Xin; Lu, Lu; Li, Haitao; Wang, Xiaohua; Lu, Hong; Jiang, Shibo; Dai, Qiu-Yun Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 9 p. 3284 - 3286

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被引用次数: 15

摘要

A series of novel 1, 4-disubstituted piperidine/piperazine derivatives were designed, synthesized and evaluated for their in vitro activities against HIV-1 Bal (R5) infection in CEMX174 5.25 M7 cells. A majority of these compounds showed potent anti-HIV-1 activities with IC50 at nanomolar levels. N-(4-Fluoro-benzyl) piperazine analog B07 hydrochloride exhibited potency against HIV-1 activity similar to that of TAK-220 hydrochloride, but it had ...