基于天然产物aphadilactonec结构关键片段的二酰基甘油酰基转移酶1抑制剂的设计与合成

doi:10.6023/cjoc201511037

	基于天然产物aphadilactonec结构关键片段的二酰基甘油酰基转移酶1抑制剂的设计与合成
	李丹 1; 尹建朋 2; 李静雅 2; 南发俊 2
刊名	有机化学
	2016
卷号	36 期号:6 页码:1359
关键词	MICE DISCOVERY OBESITY CLONING POTENT FAMILY DGAT2 aphadilactone C DGAT1 selective inhibitor PF-04620110 AZD-7687
ISSN号	0253-2786
DOI	10.6023/cjoc201511037
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]
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/286792]
专题	中国科学院上海药物研究所
作者单位	1.华东师范大学 2.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	李丹,尹建朋,李静雅,等. 基于天然产物aphadilactonec结构关键片段的二酰基甘油酰基转移酶1抑制剂的设计与合成[J]. 有机化学,2016,36(6):1359.
APA	李丹,尹建朋,李静雅,&南发俊.(2016).基于天然产物aphadilactonec结构关键片段的二酰基甘油酰基转移酶1抑制剂的设计与合成.有机化学,36(6),1359.
MLA	李丹,et al."基于天然产物aphadilactonec结构关键片段的二酰基甘油酰基转移酶1抑制剂的设计与合成".有机化学 36.6(2016):1359.