Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1364563 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
A series of C4 substituted α-ketooxazoles were examined as inhibitors of the serine hydrolase fatty acid amide hydrolase in efforts that further define and generalize a fundamental substituent effect on enzyme inhibitory potency. Thus, a plot of the Hammett σm versus −log Ki provided a linear correlation (R2 = 0.90) with a slope of 3.37 (ρ = 3.37), that is of a magnitude that indicates that of the electron-withdrawing character of the substituent dominates its effects (a one unit change in σm provides a >1000-fold change in Ki).
Graphical abstractA series of C4 substituted α-ketooxazoles were examined as inhibitors of fatty acid amide hydrolase in efforts that further define and generalize a fundamental substituent effect on enzyme inhibitory potency.Figure optionsDownload full-size imageDownload as PowerPoint slide