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.
journal_name
ACS Med Chem Lettjournal_title
ACS medicinal chemistry lettersauthors
Zimmermann SC,Rais R,Alt J,Burzynski C,Slusher BS,Tsukamoto Tdoi
10.1021/ml500335zsubject
Has Abstractpub_date
2014-10-21 00:00:00pages
1251-3issue
11issn
1948-5875journal_volume
5pub_type
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