title: Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators.
abstract: Design, synthesis and structure-activity relationships of benzimidazole derivatives as activators of the AMP-activated protein kinase (AMPK) are presented in this paper. AMPK is the central component of a protein kinase cascade that plays a key role in the regulation of energy balance. Once activated, AMPK initiates a series of responses that are aimed at restoring the energy balance of the cell and recent studies have indicated that AMPK plays an important role in regulation of the whole-body energy metabolism. The following study based on the lead compound S27847 involved modification of three regions of this compound. Preliminary structure-activity relationships are being described.
authors.affiliation: UMR CNRS 8525, Universite de Lille II, Institut de Biologie et Institut Pasteur de Lille, France. julie.charton@univ-lille2.fr
authors.forename: Julie
authors.initials: J
authors.lastname: Charton
authors.forename: Sophie
authors.initials: S
authors.lastname: Girault-Mizzi
authors.forename: Marie-Ange
authors.initials: MA
authors.lastname: Debreu-Fontaine
authors.forename: Fabienne
authors.initials: F
authors.lastname: Foufelle
authors.forename: Isabelle
authors.initials: I
authors.lastname: Hainault
authors.forename: Jean-Guy
authors.initials: JG
authors.lastname: Bizot-Espiard
authors.forename: Daniel-Henri
authors.initials: DH
authors.lastname: Caignard
authors.forename: Christian
authors.initials: C
authors.lastname: Sergheraert
mesh_terms: D055372:AMP-Activated Protein Kinases; D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001681:Biological Assay; D003510:Cyclohexanes / Q000737:chemistry*; D004734:Energy Metabolism / Q000187:drug effects; D005260:Female; D009097:Multienzyme Complexes / Q000378:metabolism*; D017346:Protein Serine-Threonine Kinases / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar
chemical_list: D001562:Benzimidazoles; D003510:Cyclohexanes; D009097:Multienzyme Complexes; C512501:S27847; D017346:Protein Serine-Threonine Kinases; D055372:AMP-Activated Protein Kinases