Optimization of the central heterocycle of α-ketoheterocycle inhibitors of fatty acid amide hydrolase

…, DG Hochstatter, I Hwang, DL Boger

Index: Kimball, F. Scott; Romero, F. Anthony; Ezzili, Cyrine; Garfunkle, Joie; Rayl, Thomas J.; Hochstatter, Dustin G.; Hwang, Inkyu; Boger, Dale L. Journal of Medicinal Chemistry, 2008 , vol. 51, # 4 p. 937 - 947

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Citation Number: 82

Abstract

The synthesis and evaluation of a refined series of α-ketoheterocycles based on the oxazole 2 (OL-135) incorporating systematic changes in the central heterocycle bearing a key set of added substituents are described. The nature of the central heterocycle, even within the systematic and minor perturbations explored herein, significantly influenced the inhibitor activity: 1, 3, 4-oxadiazoles and 1, 2, 4-oxadiazoles 9> tetrazoles, the isomeric 1, 2, 4- ...