Bioorg Med Chem Lett. 2010 Feb 1;20(3):1272-7. Epub 2009 Nov 24.

Oxime carbamate--discovery of a series of novel FAAH inhibitors.

Sit SY, Conway CM, Xie K, Bertekap R, Bourin C, Burris KD.

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Department of Chemistry, Bristol-Myers Squibb Research & Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA. sits@bms.com

Abstract

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).

PMID:: 20036536; [PubMed - indexed for MEDLINE]

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