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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

DOI: 10.1016/j.bmcl.2015.05.009