Title of article
Synthesis and biological evaluation of N-acetyl-β-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro
Author/Authors
Pi Cheng، نويسنده , , Zhiyong Jiang، نويسنده , , Rui-Rui Wang، نويسنده , , Xuemei Zhang، نويسنده , , Qian Wang، نويسنده , , Yong-Tang Zheng، نويسنده , , Jun Zhou، نويسنده , , Ji-Jun Chen، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
4476
To page
4480
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.
Keywords
N-Acetyl-?-aryl-1 , 2-didehydroethylamine , ?-Aryl-nitroolefin , NNRTIs , Anti-HIV-1 RT activity
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798446
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