title: Synthesis of kojic acid derivatives as secondary binding site probes of D-amino acid oxidase.
abstract: A series of kojic acid (5-hydroxy-2-hydroxymethyl-4H-pyran-4-one) derivatives were synthesized and tested for their ability to inhibit D-amino acid oxidase (DAAO). Various substituents were incorporated into kojic acid at its 2-hydroxymethyl group. These analogs serve as useful molecular probes to explore the secondary binding site, which can be exploited in designing more potent DAAO inhibitors.
authors.affiliation: Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, USA.
authors.forename: Mithun
authors.initials: M
authors.lastname: Raje
authors.forename: Niyada
authors.initials: N
authors.lastname: Hin
authors.forename: Bridget
authors.initials: B
authors.lastname: Duvall
authors.forename: Dana V
authors.initials: DV
authors.lastname: Ferraris
authors.forename: James F
authors.initials: JF
authors.lastname: Berry
authors.forename: Ajit G
authors.initials: AG
authors.lastname: Thomas
authors.forename: Jesse
authors.initials: J
authors.lastname: Alt
authors.forename: Camilo
authors.initials: C
authors.lastname: Rojas
authors.forename: Barbara S
authors.initials: BS
authors.lastname: Slusher
authors.forename: Takashi
authors.initials: T
authors.lastname: Tsukamoto
mesh_terms: D001665:Binding Sites / Q000187:drug effects; D003605:D-Amino-Acid Oxidase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D015335:Molecular Probes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011753:Pyrones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D015335:Molecular Probes; D011753:Pyrones; C011890:kojic acid; D003605:D-Amino-Acid Oxidase