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De-novo design and synthesis of conformationally restricted thiazolidine-2,4-dione analogues: highly selective PPAR-γ agonist in search of anti-diabetic agent
Structural Chemistry ( IF 2.1 ) Pub Date : 2020-02-17 , DOI: 10.1007/s11224-020-01500-4
Santosh S. Chhajed , Pooja E. Shinde , Sanjay J. Kshirsagar , Jayprakash N. Sangshetti , PramodKumar P. Gupta , Mala M. Parab , Debjani Dasgupta

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, 1 H-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.

中文翻译:

构象受限的噻唑烷-2,4-二酮类似物的从头设计和合成:寻找抗糖尿病药物的高选择性 PPAR-γ 激动剂

在本研究中,报道了用于选择性调节 PPAR-γ 的少数 2,4-噻唑烷二酮的设计、分子对接模拟和合成。使用细胞系分析评估少数噻唑烷-2,4-二酮的抗糖尿病活性的进一步评估。合成化合物的结构通过FT-IR、 1 H-NMR和质量分析得到确认。采用台盼蓝法和MTT法对合成的化合物进行急性毒性研究。通过葡萄糖吸收测定评估合成的化合物的抗高血糖作用。与对照相比,化合物代码 TZD4 显示出 3T3-L1 细胞吸收葡萄糖的最高百分比。
更新日期:2020-02-17
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