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Updated: Aug 11, 2025
Assessment of Mitochondrial Functions and Cell Viability in Renal Cells Overexpressing Protein Kinase C Isozymes
Published on: January 7, 2013
Imidazo[1,2-a]pyridine Derivatives as AMPK Activators: Synthesis, Structure-Activity Relationships, and Regulation of
Siming Wu1,2,3, Zhihong Xiao1,2, Junling Wei1,2
1Department of Medicinal Chemistry, Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, 410013 Hunan, P.R. China.
Abstract:
Adenosine 5'-monophosphate activated protein kinase (AMPK) has emerged as a promising target for the discovery of drugs to treat diabetic nephropathy (DN). Herein, a series of imidazo[1,2-a]pyridines were designed and synthesized. Among them, the active compound (EC50 =11.0 nM) showed good enzyme activation and molecular docking results showed hydrogen bonding interactions with the key amino acids Asn111 and Lys29 in the active site. Meanwhile, further cellular level experiments revealed that it could reduce reactive oxygen species (ROS) levels in NRK-49F cells induced by high glucose, and Western Blot experiments also demonstrate that it can increase the levels of p-AMPK and p-ACC and decrease the levels of TGF-β1. The results of this study extend the structural types of AMPK activators and provide novel lead compounds for the subsequent development.
