- Anti human immunodeficiency virus-1 (HIV-1) agents 1. Discovery of benzyl phenyl ethers as new HIV-1 inhibitors in vitro.
Anti human immunodeficiency virus-1 (HIV-1) agents 1. Discovery of benzyl phenyl ethers as new HIV-1 inhibitors in vitro.
Chemical & pharmaceutical bulletin (2009-01-06)
Hui-Ling Dai, Wu-Qing Liu, Hui Xu, Liu-Meng Yang, Min Lv, Yong-Tang Zheng
PMID19122322
摘要
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 microg/ml and therapeutic index value of 18.32. The preliminary structure-activity relationships of these benzyl phenyl ethers were also described.