950592-98-0Relevant academic research and scientific papers
Synthesis and biological evaluation of N-acetyl-β-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro
Cheng, Pi,Jiang, Zhi-Yong,Wang, Rui-Rui,Zhang, Xue-Mei,Wang, Qian,Zheng, Yong-Tang,Zhou, Jun,Chen, Ji-Jun
, p. 4476 - 4480 (2007)
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.
