29884-24-0Relevant articles and documents
A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies
Niu, Handong,Wang, Wenbao,Li, Jinyan,Lei, Yu,Zhao, Yong,Yang, Weixu,Zhao, Chaoyue,Lin, Bin,Song, Shaojiang,Wang, Shaojie
, p. 212 - 220 (2017)
A series of structurally interesting coumarin-chalcone fibrates were synthesized and evaluated for their PPARα/γ agonist activities and antioxidant activities. Among these compounds, compounds 5a, 5d, and 7a were identified as potent PPARα and γ dual agonists, and their PPARα agonist activities were found to be more potent than that of Fenofibrate. Furthermore, the results of antioxidant investigations revealed that compounds 5d and 6a?6d had greater potency than Trolox with IC50 values ranging from 9.40 μM to 18.63 μM. The structure–activity relationship revealed that the electron-withdrawing nitro group substituted at the C6′ position of the benzopyran moiety increased the PPARα and γ agonist efficacy. Moreover, the presence of a double bond on the benzopyran moiety was essential for PPARα and γ agonist efficacy. The agonist activity of PPARα exhibited by compound 5d was examined by molecular docking studies. Taken together, the results we obtained showed that compound 5d had the potential to be a lead compound for further research.
PPAR (peroxisome proliferator-activated receptor) alpha-gamma dual agonist and application thereof
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Paragraph 0116; 0117; 0118, (2018/04/28)
The invention discloses a PPAR (peroxisome proliferator-activated receptor) alpha-gamma dual agonist and an application thereof. The PPAR alpha-gamma dual agonist contains an effective quantity of a derivative represented by the formula I or the formula II in the description and a pharmaceutically acceptable salt of the derivative, wherein definition of each substituent group is as claimed in theclaims and the description. Experiments prove that the compound represented as the formula I or the formula II can remarkably improve PPAR alpha-gamma transcriptional activity and mRNA level of related target genes, has PPAR alpha-gamma dual agonist activity and can be taken as an effective component of the PPAR alpha-gamma dual agonist. The PPAR alpha-gamma dual agonist can be applied to preparation of drugs and healthy food for preventing or/and treating metabolic syndromes, particularly can be applied to preparation of drugs and healthy food for preventing or/and treating abnormal glucose metabolism or/and abnormal lipids metabolism diseases, and has broad application prospect.
Coumarin chalcone fibrates: A new structural class of lipid lowering agents
Sashidhara, Koneni V.,Palnati, Gopala Reddy,Sonkar, Ravi,Avula, Srinivasa Rao,Awasthi, Chetan,Bhatia, Gitika
, p. 422 - 431 (2013/07/27)
In our continuing search for safe and efficacious antidyslipidemic agents, structurally interesting coumarin-chalcone fibrates were synthesized and evaluated in triton WR-1339 induced hyperlipidemic rats. The most active compound 41 decreased the total cholesterol (TC), phospholipids (PL) and triglycerides (TG), of hyperlipidemic rats by 26, 24, and 25% respectively. In addition, the compound 41 significantly reversed the levels of VLDL, LDL HDL and also increased the LPL activity. Altogether, our data suggests that these novel hybrids would be a potential new class of therapeutic agents against dyslipidemia.
