Article ID Journal Published Year Pages File Type
1364563 Bioorganic & Medicinal Chemistry Letters 2008 5 Pages PDF
Abstract

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

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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