Synthesis and biological evaluation of D-amino acid oxidase inhibitors

Dana Ferraris, Bridget Duvall, Yao Sen Ko, Ajit G. Thomas, Camilo Rojas, Pavel Majer, Kenji Hashimoto, Takashi Tsukamoto

Research output: Contribution to journalArticlepeer-review

110 Scopus citations


D-Amino acid oxidase (DAAO) catalyzes the oxidation of D-amino acids including D-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[d]isoxazol-3-ol derivatives were synthesized and evaluated as DAAO inhibitors. Among them, 5-chlorobenzo[d]isoxazol-3-ol (CBIO) potently inhibited DAAO with an IC50 in the submicromolar range. Oral administration of CBIO in conjunction with D-serine enhanced the plasma and brain levels of D-serine in rats compared to the oral administration of D-serine alone.

Original languageEnglish (US)
Pages (from-to)3357-3359
Number of pages3
JournalJournal of medicinal chemistry
Issue number12
StatePublished - Jun 26 2008
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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