Background: Thiazolidinediones and its bioisostere, namely, rhodanines have become ubiquitous class of heterocyclic compounds in drug design and discovery. In the present study, as part of molecular design, a series of novel glitazones that are feasible to synthesize in our laboratory were subjected to docking studies against PPAR-γ receptor for their selection.

Methods and Results: As part of the synthesis of selected twelve glitazones, the core moiety, pyridine incorporated rhodanine was synthesized via dithiocarbamate. Later, a series of glitazones were prepared via Knovenageal condensation. In silico docking studies were performed against PPARγ protein (2PRG). The titled compounds were investigated for their cytotoxic activity against 3T3-L1 cells to identify the cytotoxicity window of the glitazones. Further, within the cytotoxicity window, glitazones were screened for glucose uptake activity against L6 cells to assess their possible antidiabetic activity.

Conclusion: Based on the glucose uptake results, structure activity relationships are drawn for the title compounds.

背景：噻唑烷二酮及其生物等排体（如罗丹酮）已成为药物设计和发现中无处不在的杂环化合物。在本研究中，作为分子设计的一部分，对在我们实验室中可行合成的一系列新型格列酮进行了针对PPAR-γ受体的对接研究，以供选择。

方法和结果：作为合成的十二个格列酮的一部分，通过二硫代氨基甲酸酯合成了核心部分，吡啶并入的罗丹宁。后来，通过Knovenageal缩合反应制备了一系列格列酮。在计算机上对PPARγ蛋白（2PRG）的对接研究。研究了标题化合物对3T3-L1细胞的细胞毒性活性，以鉴定格列酮的细胞毒性窗口。此外，在细胞毒性窗口内，筛选了格列酮对L6细胞的葡萄糖摄取活性，以评估其可能的抗糖尿病活性。

结论：根据葡萄糖吸收结果，绘制了标题化合物的结构活性关系。