Discovery and SAR development of thienopyridones: A class of small molecule AMPK activators

AMP-activated protein kinase (AMPK) is well established as a sensor and regulator of intracellular and whole-body energy metabolism. A high-throughput screen was performed in order to identify chemotypes that are bound by AMPK. A novel thienopyridone compound (1) was identified and subsequently optimized. The structure–activity relationships that emerged from this effort are described.

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