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À propos de : Delineation of a Fundamental α-Ketoheterocycle Substituent Effect for Use inthe Design of Enzyme Inhibitors        

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  • Delineation of a Fundamental α-Ketoheterocycle Substituent Effect for Use inthe Design of Enzyme Inhibitors
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  • 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.
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