Activators of 5′-AMP-activated protein kinase (AMPK) are widely used for treatment of metabolic disorders, type 2 diabetes, heart disease, anti-proliferative therapy and sports medicine. AMPK, a heterotrimeric serine/threonine protein kinase, is activated in response to reduced intracellular ATP to AMP ratio and controls numerous metabolic pathways. Activation of this kinase improves glucose uptake, fatty acid oxidation and insulin sensitivity in skeletal muscles, carbohydrate and lipid metabolism in liver and adipocytes, and release of insulin by pancreatic β cells (Long and Zierath, 2006).