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ID: ALA1777715

Journal: Bioorg Med Chem Lett

Title: Orally active aminopyridines as inhibitors of tetrameric fructose-1,6-bisphosphatase.

Authors: Hebeisen P, Haap W, Kuhn B, Mohr P, Wessel HP, Zutter U, Kirchner S, Ruf A, Benz J, Joseph C, Alvarez-Sánchez R, Gubler M, Schott B, Benardeau A, Tozzo E, Kitas E.

Abstract: A novel sulfonylureido pyridine series exemplified by compound 19 yielded potent inhibitors of FBPase showing significant glucose reduction and modest glycogen lowering in the acute db/db mouse model for Type-2 diabetes. Our inhibitors occupy the allosteric binding site and also extend into the dyad interface region of tetrameric FBPase.

CiteXplore: 21550236

DOI: 10.1016/j.bmcl.2011.04.044