In this section, you can access to the latest technical information related to the FUTURE project topic.

A novel structural class of coumarin-chalcone fibrates as PPAR?/? agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies

A series of structurally interesting coumarin-chalcone fibrates were synthesized and evaluated for their PPAR?/? agonist activities and antioxidant activities. Among these compounds, compounds 5a, 5d, and 7a were identified as potent PPAR? and ? dual agonists, and their PPAR? 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 ?M to 18.63 ?M. The structure–activity relationship revealed that the electron-withdrawing nitro group substituted at the C6? position of the benzopyran moiety increased the PPAR? and ? agonist efficacy. Moreover, the presence of a double bond on the benzopyran moiety was essential for PPAR? and ? agonist efficacy. The agonist activity of PPAR? 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.

» Author: Handong Niu, Wenbao Wang, Jinyan Li, Yu Lei, Yong Zhao, Weixu Yang, Chaoyue Zhao, Bin Lin, Shaojiang Song, Shaojie Wang

» Reference: European Journal of Medicinal Chemistry, Volume 138

» Publication Date: 29/09/2017

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