2-Substitiuted Thio- and Amino-5,8-dimethoxy-1,4-naphthoquinones as a Novel Class of Acyl-CoA: Cholestrol Acyltransferase Inhibitors
作者：
DOI: 10.5012/BKCS.2009.30.5.1088
关键词: Stereochemistry 、 IC50 、 Side chain 、 Acyl-CoA 、 Thio- 、 Structure–activity relationship 、 Carbon number 、 Chemistry 、 Acyltransferase
摘要: ,* ‡ A series of 2-alkyl or 2-arylthio-5,8-dimethoxy-1,4-naphthoquinones (2-Thio-DMNQ, 5a-s) and 2-alkylamino-5,8dimethoxy-1,4-naphthoquinones (2-Amino-DMNQ, 6a-k) was synthesized evaluated for their ACAT inhibitory activities. Among them, the 2-dodecylthio-DMNQ 5l 2-isobutylamidoundodecylthio-DMNQ 5r showed most potent activities with IC50 value 22.8 24.4 µM, respectively. In a structure-activity relationship study, 2-thio-DMNQs side chains carbon number 11 ~ 15 exhibited significant
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