Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPAR alpha selective activators
文献类型：期刊论文
| 作者 | Li, ZB; Liao, CZ; Ko, BCB; Shan, S; Tong, EHY; Yin, ZH; Pan, DS; Wong, VKW; Shi, LM; Ning, ZQ |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2004-07-05 |
| 卷号 | 14期号:13页码:3507-3511 |
| 关键词 | PPAR-alpha activators type 2 diabetes noncyclic 1 metabolic diseases 3-dicarbonyl compounds |
| ISSN号 | 0960-894X |
| 其他题名 | Bioorg. Med. Chem. Lett. |
| 中文摘要 | Lipid accumulation in nonadipose tissues is increasingly linked to the development of type 2 diabetes in obese individuals. We report here the design, synthesis, and evaluation of a series of novel PPARalpha selective activators containing 1,3-dicarbonyl moieties. Structure-activity relationship studies led to the identification of PPARalpha selective activators (compounds 10, 14, 17, 18, and 21) with stronger potency and efficacy to activate PPARalpha over PPARgamma and PPARdelta. Experiments in vivo showed that compounds 10, 14, and 17 had blood glucose lowering effect in diabetic db/db mouse model after two weeks oral dosing. The data strongly support further testing of these lead compounds in other relevant disease animal models to evaluate their potential therapeutic benefits. (C) 2004 Elsevier Ltd. All rights reserved. |
| 英文摘要 | Lipid accumulation in nonadipose tissues is increasingly linked to the development of type 2 diabetes in obese individuals. We report here the design, synthesis, and evaluation of a series of novel PPARalpha selective activators containing 1,3-dicarbonyl moieties. Structure-activity relationship studies led to the identification of PPARalpha selective activators (compounds 10, 14, 17, 18, and 21) with stronger potency and efficacy to activate PPARalpha over PPARgamma and PPARdelta. Experiments in vivo showed that compounds 10, 14, and 17 had blood glucose lowering effect in diabetic db/db mouse model after two weeks oral dosing. The data strongly support further testing of these lead compounds in other relevant disease animal models to evaluate their potential therapeutic benefits. (C) 2004 Elsevier Ltd. All rights reserved. |
| WOS标题词 | Science & Technology ; Life Sciences & Biomedicine ; Physical Sciences |
| 类目[WOS] | Chemistry, Medicinal ; Chemistry, Organic |
| 研究领域[WOS] | Pharmacology & Pharmacy ; Chemistry |
| 关键词[WOS] | AUTOMATED DOCKING ; FLEXIBLE LIGANDS ; FATTY-ACIDS ; RECEPTORS ; AGONIST ; PROTEINS ; AUTODOCK |
| 收录类别 | SCI |
| 原文出处 | |
| 语种 | 英语 |
| WOS记录号 | WOS:000221998100026 |
| 公开日期 | 2013-11-05 |
| 版本 | 出版稿 |
| 源URL | [http://ir.ipe.ac.cn/handle/122111/4914]  |
| 专题 | 过程工程研究所_研究所（批量导入） |
| 作者单位 | 1.Tsing Hua Univ, Inst Res, Chipscreen Biosci Ltd, Shenzhen 518057, Peoples R China 2.Chinese Acad Sci, Inst Proc Engn, Beijing 100080, Peoples R China 3.Univ Hong Kong, Dept Chem, Hong Kong, Hong Kong, Peoples R China 4.Univ Hong Kong, Dept Chem, Hong Kong, Hong Kong, Peoples R China 5.Univ Hong Kong, Open Lab Chem Biol, Inst Mol Technol Drug Discovery & Synth, Hong Kong, Hong Kong, Peoples R China 6.Univ Hong Kong, Inst Mol Biol, Hong Kong, Hong Kong, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, ZB,Liao, CZ,Ko, BCB,et al. Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPAR alpha selective activators[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2004,14(13):3507-3511. |
| APA | Li, ZB.,Liao, CZ.,Ko, BCB.,Shan, S.,Tong, EHY.,...&Lu, XP.(2004).Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPAR alpha selective activators.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,14(13),3507-3511. |
| MLA | Li, ZB,et al."Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPAR alpha selective activators".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 14.13(2004):3507-3511. |
入库方式： OAI收割
来源：过程工程研究所
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