Abstract
A series of 2-alkyl or 2-arylthio-5,8-dimethoxy-1,4-naphthoquinones (2-Thio-DMNQ, 5a-s) and 2-alkylamino-5,8- dimethoxy-1,4-naphthoquinones (2-Amino-DMNQ, 6a-k) was synthesized and evaluated for their ACAT inhibitory activities. Among them, the 2-dodecylthio-DMNQ 5l and 2-isobutylamidoundodecylthio-DMNQ 5r showed the most potent ACAT inhibitory activities with <TEX>$IC_{50}$</TEX> value of 22.8 and 24.4 <TEX>${\mu}M$</TEX>, respectively. In a structure-activity relationship study, 2-thio-DMNQs with side chains of carbon number 11 <TEX>$\sim$</TEX> 15 exhibited significant ACAT inhibitory activities.
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