Basic Information
ID: ALA3351460
Journal: ACS Med Chem Lett
Title: Structure-Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors.
Authors: Zimmermann SC, Rais R, Alt J, Burzynski C, Slusher BS, Tsukamoto T.
Abstract: Representative d-amino acid oxidase (DAAO) inhibitors were subjected to in vitro liver microsomal stability tests in the absence or presence of uridine diphosphate glucuronic acid (UDPGA). While carboxylate-based DAAO inhibitors displayed little glucuronidation, most DAAO inhibitors containing α-hydroxycarbonyl moiety exhibited nearly complete glucuronidation within 30 min. The one exception was 6-[2-(3,5-difluorophenyl)ethyl]-4-hydroxypyridazin-3(2H)-one 10, which exhibited some degree of resistance to glucuronidation by liver microsomes from mice, rats, and humans.
CiteXplore: 25408840
DOI: 10.1021/ml500335z
Patent ID: ┄
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