Bavachinin analogues as agonists of pan-peroxisome proliferator-activated receptors

Peroxisome proliferator-activated receptors (PPARs) agonists contribute to the regulation of glucose, lipid, and cholesterol metabolism and have emerged as key targets to treat metabolic syndrome. In our previous study, the natural compound bavachinin was found to have pan-PPAR agonist activity. In...

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Bibliographic Details
Published in:Medicinal chemistry research 2018-07, Vol.27 (7), p.1851-1862
Main Authors: Yi, Jingyu, Du, Guoxin, Zhao, Yuanyuan, Zhang, Liuqiang, Li, Bo, Zhu, Weiliang, Huang, Cheng, Li, Yiming, Guo, Fujiang
Format: Article
Language:English
Subjects:
Agonists
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Cholesterol
Glucose metabolism
Isoflavones
Lipid metabolism
Metabolic disorders
Metabolic syndrome
Metabolism
Original Research
Peroxisome proliferator-activated receptors
Pharmacology/Toxicology
Receptors
Reporter gene
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Summary:Peroxisome proliferator-activated receptors (PPARs) agonists contribute to the regulation of glucose, lipid, and cholesterol metabolism and have emerged as key targets to treat metabolic syndrome. In our previous study, the natural compound bavachinin was found to have pan-PPAR agonist activity. In this study, five isoflavones, three isoflavanones, and five scaffold-hopping analogues of bavachinin were designed, synthesised, and evaluated through reporter gene assays for pan-PPAR agonist activity. The analogue 2-(4-hydroxyphenyl)-6-isopentenyl-7-methoxy-2,3-dihydroquinolin-4(1H)-one ( 21 ) was identified as a pan-PPAR agonist, exhibiting substantially higher PPAR α/β agonist activity and equal PPAR-γ agonist activity than does bavachinin.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-018-2197-6