التفاصيل البيبلوغرافية
العنوان:
Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity
المؤلفون:
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
المصدر:
Bioorganicmedicinal chemistry letters . 22(2)
سنة النشر:
2011
مصطلحات موضوعية:
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
الوصف:
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.
تدمد:
1464-3405
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b1ef0471571a1b51d463d6743f77c74 https://pubmed.ncbi.nlm.nih.gov/22209458
Rights:
CLOSED
رقم الانضمام:
edsair.doi.dedup.....4b1ef0471571a1b51d463d6743f77c74
قاعدة البيانات:
OpenAIRE