808134-96-5Relevant articles and documents
Delineation of a fundamental α-ketoheterocycle substituent effect for use in the design of enzyme inhibitors
Romero, F. Anthony,Hwang, Inkyu,Boger, Dale L.
, p. 14004 - 14005 (2007/10/03)
The synthesis and examination of a systematic series of 5-substituted 2-keto oxazoles as inhibitors of fatty acid amide hydrolase (FAAH) defined a fundamental substituent effect that led to the discovery of inhibitors with Ki's as low as 400 pM. The intrinsic basis of the relationship (-log Ki vs σp), which relates Ki with the Hammett σp constant of the substituent, the magnitude of the effect (ρ = 3.01), and its predictive value (R2 = 0.91) suggest a widespread applicability in studies beyond FAAH. Copyright