Oxime Carbamate—Discovery of a series of novel FAAH inhibitors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(2010)

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摘要
A series of novel oxime carbamates have been identified as potent inhibitors of the key regulatory enzyme of the endocannabinoid signaling system, fatty acid amide hydrolase (FAAH). In this Letter, the rationale behind the discovery and the biological evaluations of this novel class of FAAH inhibitors are presented. Both in vitro and in vivo results of selected targets are discussed, along with inhibition kinetics and molecular modeling studies.(1) (C) 2009 Elsevier Ltd. All rights reserved.
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关键词
Oxime,Carbamate,FAAH,Inhibitor,Fatty acid amide hydrolase,Endocannabinoid,Molecular modeling,Inhibition kinetic,Signaling lipid,Cannabinoid,Anandamide,Antiinflammatory,Signal termination,Marijuana,Nociception,Pain,Tetrahydrocannabinol,Antinociceptive,Electrophilic recognition,Urea,Bisarylazole carbamates,Preclinical model,Nonprostanoid,Prostacyclin,Cholesterol,Eicosanoid,Isoprenoid,Essential fatty acid,Curtius,para-Phenoxy,Biphenyl,Reversible,Hammond's Postulate,Hargreaves,1MT5,2VYA
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