title: 6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3β inhibitors.
abstract: The synthesis and structure-activity relationships for a novel series of 6-amino-4-(pyrimidin-4-yl)pyridones derived from a high throughput screening hit are discussed. Optimization of lead matter afforded compounds with good potency, selectivity and central nervous system (CNS) exposure.
authors.affiliation: Pfizer Global Research and Development, Groton Laboratories, Groton, CT 06340, USA. karen.j.coffman@pfizer.com
authors.forename: Karen
authors.initials: K
authors.lastname: Coffman
authors.forename: Michael
authors.initials: M
authors.lastname: Brodney
authors.forename: James
authors.initials: J
authors.lastname: Cook
authors.forename: Lorraine
authors.initials: L
authors.lastname: Lanyon
authors.forename: Jayvardhan
authors.initials: J
authors.lastname: Pandit
authors.forename: Subas
authors.initials: S
authors.lastname: Sakya
authors.forename: Joel
authors.initials: J
authors.lastname: Schachter
authors.forename: Elaine
authors.initials: E
authors.lastname: Tseng-Lovering
authors.forename: Matthew
authors.initials: M
authors.lastname: Wessel
mesh_terms: D002490:Central Nervous System / Q000187:drug effects; D018360:Crystallography, X-Ray; D038341:Glycogen Synthase Kinases / Q000037:antagonists & inhibitors*; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011728:Pyridones; D038341:Glycogen Synthase Kinases