Imidazo[1,2-a]pyridine Derivatives as AMPK Activators: Synthesis, Structure–Activity Relationships, and Regulation of Reactive Oxygen Species in Renal Fibroblasts,ChemMedChem

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Imidazo[1,2-a]pyridine Derivatives as AMPK Activators: Synthesis, Structure–Activity Relationships, and Regulation of Reactive Oxygen Species in Renal Fibroblasts
ChemMedChem ( IF 3.6 ) Pub Date : 2023-02-07 , DOI: 10.1002/cmdc.202200696
Siming Wu _{1,

2,

3} , Zhihong Xiao _{1,

2} , Junling Wei _{1,

2} , Lei Zhang _{1,

3} , Yuanyuan Cao _{1,

2} , Zhuo Chen _{1,

2,

3} , Qianbin Li _{1,

2,

3} , Gaoyun Hu _{1,

2,

3}

Affiliation

Drug design efforts led to the synthesis of a series of imidazo[1,2-a]pyridines as adenosine 5′-monophosphate activated protein kinase (AMPK) activators. The most potent compound showed an EC₅₀ value of 11.0 nM against AMPK and significantly reduced ROS levels in high-glucose-induced NRK-49F cells. Western blot experiments demonstrated that this potent compound activates AMPK and affects downstream ACC, decreasing the expression level of TGF-β1.

中文翻译：

作为 AMPK 激活剂的咪唑并 [1,2-a] 吡啶衍生物：肾成纤维细胞中活性氧的合成、构效关系和调节

药物设计工作导致合成了一系列咪唑并 [1,2- a ] 吡啶作为腺苷 5'-单磷酸活化蛋白激酶 (AMPK) 激活剂。最有效的化合物对 AMPK 的 EC ₅₀值为 11.0 nM，并显着降低高葡萄糖诱导的 NRK-49F 细胞中的 ROS 水平。Western blot 实验表明，这种有效的化合物可激活 AMPK 并影响下游 ACC，从而降低 TGF-β1 的表达水平。

更新日期：2023-02-07

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