Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.
We report the discovery of a novel, chiral azetidine urea inhibitor of Fatty Acid Amide Hydrolase (FAAH,) and describe the surprising species selectivity of VER-156084 versus rat and human FAAH and also hCB1.
Hart
Terance
T
Vernalis (R&D) Ltd, Granta Park, Cambridge CB21 6GB, UK. t.hart@vernalis.com
Macias
Alba T
AT
Benwell
Karen
K
Brooks
Teresa
T
D'Alessandro
Jalanie
J
Dokurno
Pawel
P
Francis
Geraint
G
Gibbons
Ben
B
Haymes
Timothy
T
Kennett
Guy
G
Lightowler
Sean
S
Mansell
Howard
H
Matassova
Natalia
N
Misra
Anil
A
Padfield
Anthony
A
Parsons
Rachel
R
Pratt
Robert
R
Robertson
Alan
A
Walls
Steven
S
Wong
Melanie
M
Roughley
Stephen
S
D000581:Amidohydrolases / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D000818:Animals; D001384:Azetidines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D002384:Catalysis; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D051379:Mice; D018345:Mice, Knockout; D008956:Models, Chemical; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000737:chemistry; D013237:Stereoisomerism; D014508:Urea / Q000737:chemistry*; D000099252:Fatty Acid Amide Hydrolases
D000581:Amidohydrolases; D001384:Azetidines; D004791:Enzyme Inhibitors; D010880:Piperidines; D043884:Receptor, Cannabinoid, CB1; D014508:Urea; D000099252:Fatty Acid Amide Hydrolases; C545365:VER 156084; C082735:azetidine