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

…, DG Hochstatter, I Hwang, DL Boger

Index: Garfunkle, Joie; Ezzili, Cyrine; Rayl, Thomas J.; Hochstatter, Dustin G.; Hwang, Inkyu; Boger, Dale L. Journal of Medicinal Chemistry, 2008 , vol. 51, # 15 p. 4392 - 4403

Full Text: HTML

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- ...

Related Articles:

Design, synthesis, and structure− affinity relationships of novel series of sialosides as CD22-specific inhibitors

[Abdu-Allah, Hajjaj H. M.; Tamanaka, Taichi; Yu, Jie; Zhuoyuan, Lu; Sadagopan, Magesh; Adachi, Takahiro; Tsubata, Takeshi; Kelm, Soerge; Ishida, Hideharu; Kiso, Makoto Journal of Medicinal Chemistry, 2008 , vol. 51, # 21 p. 6665 - 6681]

Catalytic oxidation of alkenes with a surface-bound metalloporphyrin-peptide conjugate

[Geier III, G. Richard; Sasaki, Tomikazu Tetrahedron, 1999 , vol. 55, # 7 p. 1859 - 1870]

Structure–activity relationship of a new Series of reversible dual monoacylglycerol lipase/fatty acid amide hydrolase inhibitors

[Cisneros, Jose A.; Bjoerklund, Emmelie; Gonzalez-Gil, Ines; Hu, Yanling; Canales, Angeles; Medrano, Francisco J.; Romero, Antonio; Ortega-Gutierrez, Silvia; Fowler, Christopher J.; Lopez-Rodriguez, Maria L. Journal of Medicinal Chemistry, 2012 , vol. 55, # 2 p. 824 - 836]

More Articles...