Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity

Autor:	Hart Terance William, Rachel Parsons, Ben Gibbons, Helen Browne, Macias Alba, Heather Simmonite, Sarah Dugdale, Sean Lightowler, Howard Langh Am Mansell, Guy A. Kennett, Anthony Padfield, Geraint L. Francis, Robert M. Pratt, Teresa Brooks, Timothy Haymes, Jalanie D’Alessandro, Natalia Matassova, K Benwell, Melanie Wong, Steven B. Walls, Stephen D. Roughley, A Misra, Zoe Daniels, Angela Merrett, Alan D. Robertson, Kiri Tan
Rok vydání:	2011
Předmět:	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
Zdroj:	Bioorganicmedicinal chemistry letters. 22(2)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b1ef0471571a1b51d463d6743f77c74 https://pubmed.ncbi.nlm.nih.gov/22209458 Zobrazit plný text záznamu Full Text from ScienceDirect