Synthesis and dual PPARα/δ agonist effects of 1,4-disubstituted 1,2,3-triazole analogues of GW 501516
| Autor: | Nataša Nikolić, Calin C. Ciocoiu, Trond Vidar Hansen, Arne J. Aasen, G. Hege Thoresen, Huyen Hoa Nguyen |
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| Rok vydání: | 2010 |
| Předmět: |
Pharmacology
Agonist 1 2 3-Triazole Trifluoromethyl medicine.drug_class Stereochemistry Organic Chemistry General Medicine Triazoles PPAR agonist Thiazoles Acetic acid chemistry.chemical_compound Oleic acid chemistry COS Cells Chlorocebus aethiops Drug Discovery medicine Animals Humans PPAR alpha Luciferase PPAR delta |
| Zdroj: | European Journal of Medicinal Chemistry. 45:3047-3055 |
| ISSN: | 0223-5234 |
| DOI: | 10.1016/j.ejmech.2010.03.035 |
| Popis: | Ten 1,4-disubstituted 1,2,3-triazoles 2a – 2j were prepared and tested for their ability to increase oleic acid oxidation in human myotubes using a high-throughput multiwell assay. Compounds 2e (2-{4-[(1-(3-fluoro-4-(trifluoromethyl)phenyl)-1 H -1,2,3-triazol-4-yl)methylthio]-2-methylphenoxy}acetic acid) and 2i (2-{4-[(1-(3-chloro-4-(trifluoromethoxy)phenyl)-1 H -1,2,3-triazol-4-yl)methylthio]-2-methylphenoxy}acetic acid) exhibited potent agonist activities. Compounds 2e and 2i also exhibited powerful agonist effects for both PPARα and PPARδ in a luciferase-based assay. Consequently, these triazoles can be categorized as dual PPAR agonists. |
| Databáze: | OpenAIRE |
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