Dan Li, Jian Yin, Jing-ya Li
2016
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Quality indicators
Journal
Chinese Journal of Organic Chemistry
Abstract
Diacylglycerol acyltransferase (DGAT), the only limited enzyme in the synthesis of triacylglyc- erol (TAG), is regarded as an important therapeutic target for human obesity and other metabolic syndromes. Compounds 5-8 were designed and synthesized, which the lactone group of aphadilactone C was introduced into the PF-04620110 and AZD-7687, which have entered into the clinical research, and to verify whether the lactone in aphadilactone C played the same role as carboxylic group in PF-04620110 and AZD-7687. The final vitro assay showed that compounds 5-8 no longer have the inhibition activity to DGAT1. This might suggest that inhibition mechanism of aphadilactone C was not the same as PF-04620110 and AZD-7687 and need further study. Keywords aphadilactone C,DGAT1,selective inhibitor,PF-04620110,AZD-7687