Sun, Geng published the artcileDiscovery of AdipoRon analogues as novel AMPK activators without inhibiting mitochondrial complex I, Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is AdipoRon analog preparation AMPK mitochondrial complex I diabetes; AMPK; Activator; AdipoRon; Complex I; Hypoglycemic action.
Activation of AMPK emerges as a potential therapeutic approach to metabolic diseases. AdipoRon is claimed to be an adiponectin receptor agonist that activates AMPK through adiponectin receptor 1 (AdipoR1). However, AdipoRon also exhibits moderate inhibition of mitochondrial complex I, leading to increased risk of lactic acidosis. In order to find novel AdipoRon analogs that activate AMPK without inhibition of complex I, 27 analogs of AdipoRon were designed, synthesized and biol. evaluated. As results, benzyloxy arylamide B10 was identified as a potent AMPK activator without inhibition of complex I. B10 dose-dependently improved glucose tolerance in normal mice, and significantly lowered fasting blood glucose level and ameliorated insulin resistance in db/db diabetic mice. More importantly, unlike the pan-AMPK activator MK-8722, B10 did not cause cardiac hypertrophy, probably owing to its selective activation of AMPK in the muscle tissue but not in the heart tissue. Together, B10 represents a novel class of AMPK activators with promising therapeutic potential against metabolic disease.
European Journal of Medicinal Chemistry published new progress about AMP-activated protein kinase activators. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Name: tert-Butyl piperidin-4-ylcarbamate.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem