Anti human immunodeficiency virus-1 (HIV-1) agents 1. discovery of benzyl phenyl ethers as new HIV-1 inhibitors in vitro

Abstract

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 μg/ml and therapeutic index value of 18.32. The preliminary structure-activity relationships of these benzyl phenyl ethers were also described. © 2009 Pharmaceutical Society of Japan.