Anti human immunodeficiency virus-1 (HIV-1) agents 1. Discovery of benzyl phenyl ethers as new HIV-1 inhibitors in vitro.
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.
Dai
Hui-Ling
HL
Laboratory of Pharmaceutical Synthesis, College of Sciences, Northwest A&F University, Yangling, China.
Liu
Wu-Qing
WQ
Xu
Hui
H
Yang
Liu-Meng
LM
Lv
Min
M
Zheng
Yong-Tang
YT
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D010647:Phenyl Ethers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D019380:Anti-HIV Agents; D010647:Phenyl Ethers; C076624:dibenzyl ether