title: Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.
abstract: A series of thiadiazolopiperazinyl aryl urea fatty acid amide hydrolase (FAAH) inhibitors is described. The molecules were found to inhibit the enzyme by acting as mechanism-based substrates, forming a covalent bond with Ser241. SAR and PK properties are presented.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA.
authors.forename: John M
authors.initials: JM
authors.lastname: Keith
authors.forename: Richard
authors.initials: R
authors.lastname: Apodaca
authors.forename: Wei
authors.initials: W
authors.lastname: Xiao
authors.forename: Mark
authors.initials: M
authors.lastname: Seierstad
authors.forename: Kanaka
authors.initials: K
authors.lastname: Pattabiraman
authors.forename: Jiejun
authors.initials: J
authors.lastname: Wu
authors.forename: Michael
authors.initials: M
authors.lastname: Webb
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Karbarz
authors.forename: Sean
authors.initials: S
authors.lastname: Brown
authors.forename: Sandy
authors.initials: S
authors.lastname: Wilson
authors.forename: Brian
authors.initials: B
authors.lastname: Scott
authors.forename: Chui-Se
authors.initials: CS
authors.lastname: Tham
authors.forename: Lin
authors.initials: L
authors.lastname: Luo
authors.forename: James
authors.initials: J
authors.lastname: Palmer
authors.forename: Michelle
authors.initials: M
authors.lastname: Wennerholm
authors.forename: Sandra
authors.initials: S
authors.lastname: Chaplan
authors.forename: J Guy
authors.initials: JG
authors.lastname: Breitenbucher
mesh_terms: D000581:Amidohydrolases / Q000037:antagonists & inhibitors* / Q000172:deficiency / Q000235:genetics; D000818:Animals; D051379:Mice; D018345:Mice, Knockout; D010879:Piperazines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D013830:Thiadiazoles / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D014508:Urea / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000099252:Fatty Acid Amide Hydrolases
chemical_list: D000581:Amidohydrolases; D010879:Piperazines; D013830:Thiadiazoles; D014508:Urea; D000099252:Fatty Acid Amide Hydrolases