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ID: ALA3588827
Journal: Bioorg Med Chem Lett
Title: A new class of ghrelin O-acyltransferase inhibitors incorporating triazole-linked lipid mimetic groups.
Authors: Zhao F, Darling JE, Gibbs RA, Hougland JL.
Abstract: Inhibitors of ghrelin O-acyltransferase (GOAT) have untapped potential as therapeutics targeting obesity and diabetes. We report the first examples of GOAT inhibitors incorporating a triazole linkage as a biostable isosteric replacement for the ester bond in ghrelin and amide bonds in previously reported GOAT inhibitors. These triazole-containing inhibitors exhibit sub-micromolar inhibition of the human isoform of GOAT (hGOAT), and provide a foundation for rapid future chemical diversification and optimization of hGOAT inhibitors.
CiteXplore: 26009163