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Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity
- Source :
- Bioorganicmedicinal chemistry letters. 22(2)
- Publication Year :
- 2011
-
Abstract
- We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We describe the SAR of a series of analogues and conclude with the demonstration of in vivo dose-dependant FAAH inhibition in an anandamide-loading study in rats.
- Subjects :
- Models, Molecular
ERG1 Potassium Channel
Stereochemistry
Clinical Biochemistry
Azetidine
Pharmaceutical Science
Stereoisomerism
Biochemistry
Amidohydrolases
chemistry.chemical_compound
Structure-Activity Relationship
Cytochrome P-450 Enzyme System
Fatty acid amide hydrolase
In vivo
Drug Discovery
Structure–activity relationship
Animals
Cytochrome P-450 Enzyme Inhibitors
Humans
Urea
Enzyme Inhibitors
Molecular Biology
Dose-Response Relationship, Drug
Molecular Structure
Organic Chemistry
Anandamide
Ether-A-Go-Go Potassium Channels
Rats
nervous system
chemistry
Molecular Medicine
Azetidines
lipids (amino acids, peptides, and proteins)
psychological phenomena and processes
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 22
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....4b1ef0471571a1b51d463d6743f77c74