1096535-99-7Relevant academic research and scientific papers
Exploration of a fundamental substituent effect of α-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase
DeMartino, Jessica K.,Garfunkle, Joie,Hochstatter, Dustin G.,Cravatt, Benjamin F.,Boger, Dale L.
supporting information; experimental part, p. 5842 - 5846 (2009/05/31)
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).
