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 journalArticle

Abstract

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
Volume51
Issue number12
DOIs
StatePublished - Jun 26 2008
Externally publishedYes

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ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Ferraris, D., Duvall, B., Ko, Y. S., Thomas, A. G., Rojas, C., Majer, P., Hashimoto, K., & Tsukamoto, T. (2008). Synthesis and biological evaluation of D-amino acid oxidase inhibitors. Journal of Medicinal Chemistry, 51(12), 3357-3359. https://doi.org/10.1021/jm800200u