By using human scavenger receptor CD36 as the target, twenty-five N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their antagonistic activities for CD36-oxidatively low density lipoprotein (oxLDL) binding. The primary analysis of structure–activity relationship (SAR) indicated a methoxyl at the 7-position and a hydroxyl at the 6-or 8-position could afford good activities. Among these analogs, compounds 7e ...