title: Glucokinase-activating ureas.
abstract: The synthesis, SAR and biological evaluation of a series of ureas that activate glucokinase, a target for diabetes therapy as a result of its critical role in the regulation of whole-body glucose homeostasis, are described. Some of the urea-containing glucokinase activators lowered blood glucose levels in vivo following oral dosing to C57BL/6J mice.
authors.affiliation: OSI Pharmaceuticals, 1 Bioscience Park Drive, Farmingdale, NY 11735, USA.
authors.forename: Arlindo L
authors.initials: AL
authors.lastname: Castelhano
authors.forename: Hanqing
authors.initials: H
authors.lastname: Dong
authors.forename: Matthew C T
authors.initials: MC
authors.lastname: Fyfe
authors.forename: Lisa S
authors.initials: LS
authors.lastname: Gardner
authors.forename: Yukari
authors.initials: Y
authors.lastname: Kamikozawa
authors.forename: Satomi
authors.initials: S
authors.lastname: Kurabayashi
authors.forename: Masao
authors.initials: M
authors.lastname: Nawano
authors.forename: Rikiya
authors.initials: R
authors.lastname: Ohashi
authors.forename: Martin J
authors.initials: MJ
authors.lastname: Procter
authors.forename: Li
authors.initials: L
authors.lastname: Qiu
authors.forename: Chrystelle M
authors.initials: CM
authors.lastname: Rasamison
authors.forename: Karen L
authors.initials: KL
authors.lastname: Schofield
authors.forename: Vilas K
authors.initials: VK
authors.lastname: Shah
authors.forename: Kiichiro
authors.initials: K
authors.lastname: Ueta
authors.forename: Geoffrey M
authors.initials: GM
authors.lastname: Williams
authors.forename: David
authors.initials: D
authors.lastname: Witter
authors.forename: Kosuke
authors.initials: K
authors.lastname: Yasuda
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects / Q000378:metabolism; D003920:Diabetes Mellitus / Q000188:drug therapy / Q000378:metabolism; D004789:Enzyme Activation / Q000187:drug effects; D005941:Glucokinase / Q000187:drug effects* / Q000378:metabolism*; D006706:Homeostasis / Q000187:drug effects / Q000502:physiology; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D001786:Blood Glucose; D014508:Urea; D005941:Glucokinase