De-novo design and synthesis of conformationally restricted thiazolidine-2,4-dione analogues: highly selective PPAR-gamma agonist in search of anti-diabetic agent

STRUCTURAL CHEMISTRY(2020)

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摘要
In the present investigation, design, molecular docking simulations, and synthesis of few 2,4-thiazolidinedione for selective modulation of PPAR-gamma are reported. Further evaluation of anti-diabetic activity of few thiazolidine-2,4-diones is assessed using cell line analysis. The structures of the synthesized compounds were confirmed on the basis of FT-IR, H-1-NMR, and mass analyses. Acute toxicity study was done to by using Trypan blue assay and MTT assay of the synthesized compounds. Synthesized compounds were evaluated for their antihyperglycemic effect by glucose absorption assay. The compound code TZD4 showed highest percentage of glucose absorption by 3T3-L1 cells compared with control.
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关键词
Type 2 diabetes,Molecular docking,Conformationally restricted TZD,Cell line analysis
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