Microwave-assisted efficient synthesis of pyrazole-fibrate derivatives as stimulators of glucose uptake in skeletal muscle cells
| Autor: | Koneni V. Sashidhara, Shubham Pandey, L. Ravithej Singh, Sampa Gupta, Amit K. Rai, Akhilesh K. Tamrakar, Ruchir Kant |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
medicine.drug_class
Glucose uptake Clinical Biochemistry Pharmaceutical Science Stimulation Fibrate Pyrazole 01 natural sciences Biochemistry Structure-Activity Relationship chemistry.chemical_compound Pyrimidinones Drug Discovery medicine Animals Microwaves Muscle Skeletal Molecular Biology Dose-Response Relationship Drug Molecular Structure biology 010405 organic chemistry Myogenesis Organic Chemistry Fibric Acids Skeletal muscle Rats 0104 chemical sciences 010404 medicinal & biomolecular chemistry Glucose medicine.anatomical_structure chemistry biology.protein Pyrazoles Molecular Medicine GLUT4 |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 34:127760 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2020.127760 |
| Popis: | The design and synthesis of a series of pyrazolo[3,4-d]pyrimidinones containing fibrate side chains have been accomplished by utilizing the concept of molecular hybridization. All the synthesized compounds were evaluated for the glucose uptake stimulatory effect in L6 rat skeletal muscle cells. Four compounds (3f, 3g, 3j and 3q) were found to show significant stimulation of glucose uptake. Further these four compounds have been examined for their Glut4 translocation stimulatory effect in L6-Glut4myc myotubes. Compound 3q was found to exert maximum increase in GLUT4myc translocation. |
| Databáze: | OpenAIRE |
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