期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 12, 期 11, 页码 1783-1786出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.1c00400
关键词
Prenylated benzopyrans; Horner-Wadsworth-Emmons reaction; PPAR alpha/gamma activity
资金
- Generalitat Valencia [APOTIP/2020/011]
- Carlos III Health Institute (ISCIII)
- European Regional Development Fund [CP15/00150, PI18/01450]
- Agence Nationale pour la Recherche [ANR-10 LABX-0046]
- ERC Avanced Grant [694717]
- European Social Fund [CP15/00150, CPII20/00010]
- ISCIII [FI19/00153]
- European Research Council (ERC) [694717] Funding Source: European Research Council (ERC)
A series of 2-prenylated benzopyrans were synthesized as analogues of the natural dual PPAR alpha/gamma agonist polycerasoidol, showing high efficacy in activating both hPPAR alpha and hPPAR gamma. These compounds have the potential to be lead compounds for preventing cardiometabolic diseases.
We have synthesized series of 2-prenylated benzopyrans as analogues of the natural polycerasoidol, a dual PPAR alpha/gamma agonist with anti-inflammatory effects. The prenylated side chain consists of five or nine carbons with an alpha-alkoxy-alpha,beta-unsaturated ester moiety. Prenylation was introduced via the Grignard reaction, followed by Johnson-Claisen rearrangement, and the alpha-alkoxy-alpha,beta-unsaturated ester moiety was introduced by the Horner-Wadsworth-Emmons reaction. Synthetic derivatives showed high efficacy to activate both hPPAR alpha and hPPAR gamma as dual PPAR alpha/gamma agonists. These prenylated benzopyrans emerge as lead compounds potentially useful for preventing cardiometabolic diseases.
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