Back to Search
Start Over
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors
- Source :
- Bioorganic & Medicinal Chemistry. 21:28-41
- Publication Year :
- 2013
- Publisher :
- Elsevier BV, 2013.
-
Abstract
- A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the lead compound 3 to improve its DMPK profile as well as in vitro potency. We identified the thiazole compound 60j with potent inhibitory activity, high brain permeability, and good bioavailability. Compound 60j showed a potent and dose-dependent anti-nociceptive effect in the acetic acid-induced writhing test in mice.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Pain
Pharmaceutical Science
Biochemistry
Piperazines
Amidohydrolases
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Fatty acid amide hydrolase
Drug Discovery
Animals
Humans
Urea
Potency
Thiazole
Piperazine
Molecular Biology
Biological evaluation
Analgesics
Organic Chemistry
In vitro
Rats
Bioavailability
Molecular Docking Simulation
Thiazoles
chemistry
Molecular Medicine
Lead compound
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....02fe0e6423f9c80cdc30c75070da14d9