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Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase
- Source :
- Bioorganic & Medicinal Chemistry Letters. 24:737-741
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- A series of mechanism based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with spirocyclic diamine cores is described. A potent member of this class, (37), was found to inhibit FAAH centrally, elevate the brain levels of three fatty acid ethanolamides [FAAs: anandamide (AEA), oleoyl ethanolamide (OEA) and palmitoyl ethanolamide (PEA)], and was moderately efficacious in a rat model of neuropathic pain.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Administration, Oral
Pharmaceutical Science
Diamines
Biochemistry
Amidohydrolases
chemistry.chemical_compound
Heterocyclic Compounds
Fatty acid amide hydrolase
Diamine
Drug Discovery
Hydrolase
Animals
Urea
Ethanolamide
Spiro Compounds
Molecular Biology
chemistry.chemical_classification
Molecular Structure
Organic Chemistry
Brain
Fatty acid
Serine hydrolase
Anandamide
Endocannabinoid system
Rats
Enzyme Activation
chemistry
Cyclization
Azetidines
Molecular Medicine
lipids (amino acids, peptides, and proteins)
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 24
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....c4908988252b5adc440f435416fadbcc
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.12.113