Synthesis of kojic acid derivatives as secondary binding site probes of D-amino acid oxidase

  • Bioorg Med Chem Lett. 2013 Jul 1;23(13):3910-3. doi: 10.1016/j.bmcl.2013.04.062.
Mithun Raje  1 ,  Niyada Hin ,  Bridget Duvall ,  Dana V Ferraris ,  James F Berry ,  Ajit G Thomas ,  Jesse Alt ,  Camilo Rojas ,  Barbara S Slusher ,  Takashi Tsukamoto
Affiliations
  • 1. Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, USA.
PMID: 23683589 DOI: 10.1016/j.bmcl.2013.04.062
Abstract

A series of kojic acid (5-hydroxy-2-hydroxymethyl-4H-pyran-4-one) derivatives were synthesized and tested for their ability to inhibit D-Amino acid oxidase (DAAO). Various substituents were incorporated into kojic acid at its 2-hydroxymethyl group. These analogs serve as useful molecular probes to explore the secondary binding site, which can be exploited in designing more potent DAAO inhibitors.