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

Gang Zhao; Rajesh R Iyengar; Andrew S Judd; Barbara Cool; William Chiou; Lemma Kifle; Ernst Frevert; Hing Sham; Philip R Kym

doi:10.1016/j.bmcl.2007.04.011

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

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3254-7. doi: 10.1016/j.bmcl.2007.04.011. Epub 2007 Apr 10.

Authors

Gang Zhao¹, Rajesh R Iyengar, Andrew S Judd, Barbara Cool, William Chiou, Lemma Kifle, Ernst Frevert, Hing Sham, Philip R Kym

Affiliation

¹ Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. [email protected]

PMID: 17451949
DOI: 10.1016/j.bmcl.2007.04.011

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.

MeSH terms

AMP-Activated Protein Kinases
Biological Assay
Energy Metabolism / drug effects*
Energy Metabolism / physiology
Enzyme Activation / drug effects*
Enzyme Activation / physiology
Enzyme Activators / chemistry
Enzyme Activators / pharmacology*
Multienzyme Complexes / metabolism*
Protein Serine-Threonine Kinases / metabolism*
Pyridines / chemistry
Pyridines / pharmacology*
Structure-Activity Relationship

Substances

Enzyme Activators
Multienzyme Complexes
Pyridines
thienopyridine
Protein Serine-Threonine Kinases
AMP-Activated Protein Kinases