Journal
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 57, Issue 1, Pages 84-86Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.57.84
Keywords
benzyl phenyl ether; human immunodeficiency virus; inhibitor
Funding
- New Century Excellent University Talents, State Education Ministry of China [NCET-06-0868]
- Key Project of Chinese Ministry of Education [107105]
- Research Fund for the Doctoral Program of Higher Education of China [20070712025]
- Key Scientific and Technological projects of Yunnan province [2004NG12]
- National 973 project of China [2006CB504200]
- Knowledge Innovation Program of CAS [KSCX1-YW-R-24]
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Ten single benzyl phenyl ethers were synthesized and evaluated as human immunodeficiency virus-1 (HIV-1) inhibitors in vitro for the first time. Among these compounds, especially 4-nitrobenzyl phenyl ether (3h) exhibited the highest anti-HIV-1 activity with EC50 (concentration of drug that reduces syncytia formation by 50%) value of 5.96 mu g/ml and therapeutic index value of 18.32. The preliminary structure-activity relationships of these benzyl phenyl ethers were also described.
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