Discovery and SAR development of thienopyridones: a class of small molecule AMPK activators
- Resource Type
- Authors
- Andrew S. Judd; Lemma Kifle; Barbara L. Cool; Rajesh R. Iyengar; Hing L. Sham; Ernst U. Frevert; William J. Chiou; Gang Zhao; Philip R. Kym
- Source
- Bioorganicmedicinal chemistry letters. 17(12)
- Subject
- Pyridines
Clinical Biochemistry
Regulator
Pharmaceutical Science
Enzyme Activators
AMP-Activated Protein Kinases
Protein Serine-Threonine Kinases
Biochemistry
Structure-Activity Relationship
AMP-activated protein kinase
Multienzyme Complexes
Drug Discovery
Structure–activity relationship
Protein kinase A
Molecular Biology
biology
Chemistry
Activator (genetics)
Organic Chemistry
AMPK
Small molecule
Enzyme Activation
biology.protein
Molecular Medicine
Biological Assay
Signal transduction
Energy Metabolism
- Language
- ISSN
- 0960-894X
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.