Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C

doi:10.6023/cjoc201511037

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	Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C
	Li Dan 1; Yin Jianpeng 2; Li Jingya2 ; Nan Fajun2
刊名	CHINESE JOURNAL OF ORGANIC CHEMISTRY
	2016-06-25
卷号	36 期号:6 页码:1359-1367
关键词	aphadilactone C DGAT1 selective inhibitor PF-04620110 AZD-7687
ISSN号	0253-2786
DOI	10.6023/cjoc201511037
文献子类	Article
英文摘要	Diacylglycerol acyltransferase (DGAT), the only limited enzyme in the synthesis of triacylglycerol (TAG), is regarded as an important therapeutic target for human obesity and other metabolic syndromes. Compounds 5 similar to 8 were designed and synthesized, in which the lactone group of aphadilactone C was introduced into the PF-04620110 and AZD-7687, which have entered into the clinical research, 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 similar to 8 have not the inhibition activity to DGAT1. This might suggest that inhibition mechanism of aphadilactone C was not the same as PF-04620110 and AZD-7687.
资助项目	Shanghai Key Laboratory of Psychotic Disorders[13DZ226050014K-10]
WOS关键词	TRIGLYCERIDE SYNTHESIS ; OBESITY RESISTANCE ; MICE ; DISCOVERY ; CLONING ; POTENT ; FAMILY ; DGAT2
WOS研究方向	Chemistry
语种	中文
CSCD记录号	CSCD:5748046
出版者	SCIENCE PRESS
WOS记录号	WOS:000384603800018
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275985]
专题	国家新药筛选中心中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Nan Fajun
作者单位	1.East China Normal Univ, Coll Chem & Mol Engn, Shanghai 200062, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Li Dan,Yin Jianpeng,Li Jingya,et al. Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2016,36(6):1359-1367.
APA	Li Dan,Yin Jianpeng,Li Jingya,&Nan Fajun.(2016).Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C.CHINESE JOURNAL OF ORGANIC CHEMISTRY,36(6),1359-1367.
MLA	Li Dan,et al."Design and Synthesis of Diacylglycerol Acyltransferase 1 Inhibitors Based on Aphadilactone C".CHINESE JOURNAL OF ORGANIC CHEMISTRY 36.6(2016):1359-1367.