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首页> 外文期刊>Structural Chemistry >De-novo design and synthesis of conformationally restricted thiazolidine-2,4-dione analogues: highly selective PPAR-gamma agonist in search of anti-diabetic agent
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De-novo design and synthesis of conformationally restricted thiazolidine-2,4-dione analogues: highly selective PPAR-gamma agonist in search of anti-diabetic agent

机译:De-Novo设计和合成构象限制的噻唑烷-2,4-二酮类似物:高选择性PPAR-γ激动剂寻找抗糖尿病剂

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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.
机译:报道了在本发明的研究中,据报道,少数2,4-噻唑烷基的设计,分子对接模拟和合成用于PPAR-γ的选择性调节。 使用细胞系分析评估少量噻唑烷-2,4-致噻吩的抗糖尿病活性的进一步评价。 在FT-IR,H-1-NMR和质量分析的基础上证实了合成化合物的结构。 通过使用合成化合物的台盼蓝测定和MTT测定来完成急性毒性研究。 通过葡萄糖吸收测定评价合成化合物的抗血糖作用。 复合码TZD4与3T3-L1细胞与对照相比,3T3-L1细胞显示出最高百分比的葡萄糖吸收。

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