Oxime Carbamate-Discovery of a series of novel FAAH inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 3, 2010, Pages 1272-1277

  Sit, S Y ^a   Conway, Charles M ^a   Xie, Kai ^a   Bertekap, Robert ^a   Bourin, Clotilde ^a   Burris, Kevin D ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

1MT5; 2VYA; Anandamide; Antiinflammatory; Antinociceptive; Biphenyl; Bisarylazole carbamates; Cannabinoid; Carbamate; Cholesterol; Curtius; Eicosanoid; Electrophilic recognition; Endocannabinoid; Essential fatty acid; FAAH; Fatty acid amide hydrolase; Hammond's Postulate; Hargreaves; Inhibition kinetic; Inhibitor; Isoprenoid; Marijuana; Molecular modeling; Nociception; Nonprostanoid; Oxime; Pain; para Phenoxy; Preclinical model; Prostacyclin; Reversible; Signal termination; Signaling lipid; Tetrahydrocannabinol; Urea

Indexed keywords

ANANDAMIDE; ANTINOCICEPTIVE AGENT; CARBAMIC ACID DERIVATIVE; CARBON; FATTY ACID AMIDASE; FATTY ACID AMIDASE INHIBITOR; MORPHINE SULFATE; OXIME DERIVATIVE; AMIDASE; CANNABINOID RECEPTOR AFFECTING AGENT; FATTY-ACID AMIDE HYDROLASE; OXIME; PROTEIN BINDING;

ANIMAL EXPERIMENT; ANTINOCICEPTION; ARTICLE; CONTROLLED STUDY; DRUG SCREENING; ENZYME INHIBITION; IC 50; IN VITRO STUDY; IN VIVO STUDY; MOLECULAR DOCKING; MOLECULAR MODEL; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; CELL LINE; CHEMISTRY; COMPARATIVE STUDY; DRUG DEVELOPMENT; DRUG EFFECTS; HUMAN; METABOLISM; PHYSIOLOGY; PROCEDURES; PROTEIN TERTIARY STRUCTURE; SIGNAL TRANSDUCTION; X RAY CRYSTALLOGRAPHY;

AMIDOHYDROLASES; ANIMALS; CARBAMATES; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; ENDOCANNABINOIDS; HUMANS; OXIMES; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; RATS; SIGNAL TRANSDUCTION; CANNABINOID RECEPTOR MODULATORS;

CANNABIS SATIVA;

EID: 74049130981     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.11.080     Document Type: Article

References (31)

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30. max values with increasing inhibitor concentration.
31. H4 cells that express transfected human FAAH were used for all in vitro experiments. See Ref. 4 for details.