6-Hydroxy-1, 2, 4-triazine-3, 5 (2 H, 4 H)-dione Derivatives as Novel d-Amino Acid Oxidase Inhibitors

…, B Duvall, D Ferraris, J Alt, AG Thomas…

Index: Berry, James F.; Rais, Rana; Slusher, Barbara S.; Tsukamoto, Takashi; Ferraris, Dana V.; Duvall, Bridget; Hin, Niyada; Alt, Jesse; Thomas, Ajit G.; Rojas, Camilo; Hashimoto, Kenji Medicinal Chemistry letters, 2012 , vol. 3, # 10 p. 839 - 843,5 Title/Abstract Full Text Show Details Berry, James F.; Ferraris, Dana V.; Duvall, Bridget; Hin, Niyada; Rais, Rana; Alt, Jesse; Thomas, Ajit G.; Rojas, Camilo; Hashimoto, Kenji; Slusher, Barbara S.; Tsukamoto, Takashi ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 10 p. 839 - 843

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Citation Number: 4

Abstract

A series of 2-substituted 6-hydroxy-1, 2, 4-triazine-3, 5 (2 H, 4 H)-dione derivatives were synthesized as inhibitors of d-amino acid oxidase (DAAO). Many compounds in this series were found to be potent DAAO inhibitors, with IC50 values in the double-digit nanomolar range. The 6-hydroxy-1, 2, 4-triazine-3, 5 (2 H, 4 H)-dione pharmacophore appears metabolically resistant to O-glucuronidation unlike other structurally related DAAO ...