title: Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators.
abstract: The identification and structure-activity-relationships (SARs) of novel 2-amino benzamide glucokinase activators are described. Compounds in this series were developed to be potent GK activators, and their binding mode to the GK protein was determined by crystal structure analysis. In vivo pharmacokinetic and acute in vivo efficacy studies of compound 18 are also described.
authors.affiliation: Banyu Tsukuba Research Institute, Banyu Pharmaceutical Co. Ltd., Okubo-3, Tsukuba, 300-2611 Ibaraki, Japan.
authors.forename: Teruyuki
authors.initials: T
authors.lastname: Nishimura
authors.forename: Tomoharu
authors.initials: T
authors.lastname: Iino
authors.forename: Morihiro
authors.initials: M
authors.lastname: Mitsuya
authors.forename: Makoto
authors.initials: M
authors.lastname: Bamba
authors.forename: Hitomi
authors.initials: H
authors.lastname: Watanabe
authors.forename: Daisuke
authors.initials: D
authors.lastname: Tsukahara
authors.forename: Kenji
authors.initials: K
authors.lastname: Kamata
authors.forename: Kaori
authors.initials: K
authors.lastname: Sasaki
authors.forename: Sumika
authors.initials: S
authors.lastname: Ohyama
authors.forename: Hideka
authors.initials: H
authors.lastname: Hosaka
authors.forename: Mayumi
authors.initials: M
authors.lastname: Futamura
authors.forename: Yasufumi
authors.initials: Y
authors.lastname: Nagata
authors.forename: Jun-Ichi
authors.initials: J
authors.lastname: Eiki
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects / Q000502:physiology; D000818:Animals; D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites / Q000187:drug effects / Q000502:physiology; D004789:Enzyme Activation / Q000187:drug effects / Q000502:physiology; D005941:Glucokinase / Q000378:metabolism*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
chemical_list: D001549:Benzamides; D005941:Glucokinase