ArticleBioorganic & medicinal chemistry letters2016
D-Amino acid oxidase inhibitors based on the 5-hydroxy-1,2,4-triazin-6(1H)-one scaffold.
Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
6 citing papers in PubMed, 12 citations in OpenAlex.
- Promising Application of D-Amino Acids toward Clinical Therapy.International journal of molecular sciences · 2022Review
- Synthesis and Biochemical Evaluation of Lid-Open D-Amino Acid Oxidase Inhibitors.Molecules (Basel, Switzerland) · 2019Article
- Chronic d-serine supplementation impairs insulin secretion.Molecular metabolism · 2018Article
- Molecular modeling studies of 1,2,4-triazine derivatives as novel h-DAAO inhibitors by 3D-QSAR, docking and dynamics simulations.RSC advances · 2018Article
- Competitive Inhibitors Unveil Structure/Function Relationships in Human D-Amino Acid Oxidase.Frontiers in molecular biosciences · 2017Review
- Mouse d-Amino-Acid Oxidase: Distribution and Physiological Substrates.Frontiers in molecular biosciences · 2017Review
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
A series of 3-substituted 5-hydroxy-1,2,4-triazin-6(1H)-one derivatives were designed and synthesized as a new class of d-amino acid oxidase (DAAO) inhibitors. Some of the newly synthesized derivatives showed potent inhibitory activity against human DAAO with IC50 values in the nanomolar range. Among them, 6-hydroxy-3-phenethyl-1,2,4-triazin-5(2H)-one 6b and 3-((6-fluoronaphthalen-2-yl)methylthio)-6-hydroxy-1,2,4-triazin-5(2H)-one 6m were found to be metabolically stable in mouse liver microsomes. In addition, compound 6b was found to be orally available in mice and able to enhance plasma d-serine levels following its co-administration with d-serine compared to the oral administration of d-serine alone.
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Registered trials
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