Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators
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Published on: January 22, 2019
Julie Charton1, Sophie Girault-Mizzi, Marie-Ange Debreu-Fontaine
1UMR CNRS 8525, Universite de Lille II, Institut de Biologie et Institut Pasteur de Lille, France. julie.charton@univ-lille2.fr
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.
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