134071-03-7Relevant academic research and scientific papers
Discovery of a potent, selective, and efficacious class of reversible α-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics
Boger, Dale L.,Miyauchi, Hiroshi,Du, Wu,Hardouin, Christophe,Fecik, Robert A.,Cheng, Heng,Hwang, Inkyu,Hedrick, Michael P.,Leung, Donmienne,Acevedo, Orlando,Guimar?es, Cristiano R. W.,Jorgensen, William L.,Cravatt, Benjamin F.
, p. 1849 - 1856 (2007/10/03)
Fatty acid amide hydrolase (FAAH) degrades neuromodulating fatty acid amides including anandamide (endogenous cannabinoid agonist) and oleamide (sleep-inducing lipid) at their sites of action and is intimately involved in their regulation. Herein we report the discovery of a potent, selective, and efficacious class of reversible FAAH inhibitors that produce analgesia in animal models validating a new therapeutic target for pain intervention. Key to the useful inhibitor discovery was the routine implementation of a proteomics-wide selectivity screen against the serine hydrolase superfamily ensuring selectivity for FAAH coupled with systematic in vivo examinations of candidate inhibitors.
AN UMPOLUNG OF ARYL AND VINYL HALIDES USING TRIS-(TRIMETHYLSILYL)ALUMINUM AND APROACH TO META- AND PARA-BRIDGED AROMATICS
Trost, Barry M.,Yoshida, Jun-ichi
, p. 4895 - 4898 (2007/10/02)
Nickel and palladium catalysts effect the chemoselective and stereocontrolled umpolung of aryl and vinyl halides to trimethylsilyl derivatives; this reaction permits a regioselective approach to cyclophanes.
