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
文献类型：期刊论文
| 作者 | 李丹1; 尹建朋2; 李静雅2 ; 南发俊2
|
| 刊名 | 有机化学
 |
| 出版日期 | 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 |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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