Structure–Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors | Zendy

Sarah C. Zimmermann | Zendy; Rana Rais | Zendy; Jesse Alt | Zendy; Caitlin Burzynski | Zendy; Barbara S. Slusher | Zendy; Takashi Tsukamoto | Zendy

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Structure–Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors

Author(s) -

Sarah C. Zimmermann,

Rana Rais,

Jesse Alt,

Caitlin Burzynski,

Barbara S. Slusher,

Takashi Tsukamoto

Publication year - 2014

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml500335z

Subject(s) - glucuronidation , microsome , biochemistry , oxidase test , chemistry , glucuronic acid , enzyme , uridine diphosphate , glycosyltransferase , glucuronosyltransferase , uridine , moiety , metabolism , stereochemistry , rna , polysaccharide , gene

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.

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