| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377396 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
A variety of N-acetyl-β-aryl-1,2-didehydroethylamines were synthesized by direct reduction–acetylation of β-aryl-nitroolefins and assayed as HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the first time. Compound 7a exhibited a TI value of >13.2 with CC50 value of >0.787 mM in C8166 cells. This structure–activity relationship (SAR) study provided a new lead for design and discovery of more potent and selective analogues act as NNRTIs.
Graphical abstractCompounds 4 and 7 were assayed as NNRTIs against HIV-1 for the first time. Compound 7a (Ar = 2-Br-phenyl) exhibited a TI value of >13.2 (CC50 > 0.787 mM) in C8166 cells.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Pi Cheng, Zhi-Yong Jiang, Rui-Rui Wang, Xue-Mei Zhang, Qian Wang, Yong-Tang Zheng, Jun Zhou, Ji-Jun Chen,