title: Discovery and SAR development of thienopyridones: a class of small molecule AMPK activators.
abstract: 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.
authors: Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. zhaoxing2@yahoo.com
authors: Gang
authors: G
authors: Zhao
authors: Rajesh R
authors: RR
authors: Iyengar
authors: Andrew S
authors: AS
authors: Judd
authors: Barbara
authors: B
authors: Cool
authors: William
authors: W
authors: Chiou
authors: Lemma
authors: L
authors: Kifle
authors: Ernst
authors: E
authors: Frevert
authors: Hing
authors: H
authors: Sham
authors: Philip R
authors: PR
authors: Kym
mesh_terms: D055372:AMP-Activated Protein Kinases; D001681:Biological Assay; D004734:Energy Metabolism / Q000187:drug effects* / Q000502:physiology; D004789:Enzyme Activation / Q000187:drug effects* / Q000502:physiology; D020536:Enzyme Activators / Q000737:chemistry / Q000494:pharmacology*; D009097:Multienzyme Complexes / Q000378:metabolism*; D017346:Protein Serine-Threonine Kinases / Q000378:metabolism*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D020536:Enzyme Activators; D009097:Multienzyme Complexes; D011725:Pyridines; C446540:thienopyridine; D017346:Protein Serine-Threonine Kinases; D055372:AMP-Activated Protein Kinases