Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368971 | Bioorganic & Medicinal Chemistry Letters | 2015 | 4 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Feifei Zhao, Joseph E. Darling, Richard A. Gibbs, James L. Hougland,