Synthesis of novel imbricatolic acid analogues via insertion of N-substituted piperazine at C-15/C-19 positions, displaying glucose uptake stimulation in L6 skeletal muscle cells
| Autor: | Padam Kumar, Rakesh Maurya, Arvind K. Srivastava, Mohammad Faheem Khan, Akhilesh K. Tamrakar, Jyotsana Pandey |
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| Rok vydání: | 2012 |
| Předmět: |
Stereochemistry
Glucose uptake Clinical Biochemistry Pharmaceutical Science Stimulation Biochemistry Piperazines Cell Line Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Animals Muscle Skeletal Piperazine Molecular Biology Muscle Cells Molecular Structure Organic Chemistry Skeletal muscle In vitro Rats Glucose medicine.anatomical_structure chemistry Yield (chemistry) Molecular Medicine Diterpenes Diterpene Lead compound |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 22:4636-4639 |
| ISSN: | 0960-894X |
| Popis: | A new class of N-substituted piperazine analogues of imbricatolic acid have been designed and synthesized by using the appropriate synthetic routes in excellent yield. All synthesised compounds were screened for their in vitro glucose uptake stimulatory activity. Among them compounds 4b, 4e, 8b, and 8e triggered L6 skeletal muscle cells for glucose uptake at 54.73%, 40.79%, 40.90%, and 39.55% stimulation, respectively. Compound 4b has emerged as important lead compound showing potential antidiabetic activity. Illustration about their synthesis and in vitro glucose uptake activity is described. |
| Databáze: | OpenAIRE |
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