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Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPAR alpha selective activators
Alternative TitleBioorg. Med. Chem. Lett.
Li, ZB; Liao, CZ; Ko, BCB; Shan, S; Tong, EHY; Yin, ZH; Pan, DS; Wong, VKW; Shi, LM; Ning, ZQ; Hu, WM; Zhou, JJ; Chung, SSM; Lu, XP
2004-07-05
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
Volume14Issue:13Pages:3507-3511
AbstractLipid 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.; 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.
KeywordPpar-alpha Activators Type 2 Diabetes Noncyclic Metabolic Diseases 1 3-dicarbonyl Compounds
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences
DOI10.1016/j.bmcl.2004.04.053
URL查看原文
Indexed BySCI
Language英语
WOS KeywordAUTOMATED DOCKING ; FLEXIBLE LIGANDS ; FATTY-ACIDS ; RECEPTORS ; AGONIST ; PROTEINS ; AUTODOCK
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS SubjectChemistry, Medicinal ; Chemistry, Organic
WOS IDWOS:000221998100026
Citation statistics
Cited Times:19[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Version出版稿
Identifierhttp://ir.ipe.ac.cn/handle/122111/4914
Collection研究所(批量导入)
Affiliation1.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
Recommended Citation
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.
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