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1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase
- Source :
- Bioorganic & Medicinal Chemistry Letters. 24:1280-1284
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was efficacious in a rat model of neuropathic pain.
- Subjects :
- Stereochemistry
education
Clinical Biochemistry
Rat model
Pharmaceutical Science
Plasma protein binding
Biochemistry
Amidohydrolases
Structure-Activity Relationship
chemistry.chemical_compound
Fatty acid amide hydrolase
Catalytic Domain
Drug Discovery
Animals
Humans
Structure–activity relationship
Enzyme Inhibitors
Binding site
Molecular Biology
chemistry.chemical_classification
Analgesics
Binding Sites
Aryl
Organic Chemistry
Target engagement
Brain
Amino Alcohols
humanities
Rats
Molecular Docking Simulation
Disease Models, Animal
Pyrimidines
Enzyme
chemistry
Neuralgia
Molecular Medicine
Half-Life
Protein Binding
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 24
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....dc169c27063de79ede8ba3a615dade39