Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
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4-Hydroxy-6-Oxo-6,7-Dihydro-Thieno[2,3-b] Pyrimidine Derivatives : Synthesis and Their Biological Evaluation for the Glycine Site Acting on the N-Methyl-D-Aspartate (NMDA) Receptor

  • Hwang, Ki-Jun (Department of Chemistry and Research Center of Bioactive Materials, College of Natural Science) ;
  • Lee, Tae-Suk (Department of Chemistry and Research Center of Bioactive Materials, College of Natural Science) ;
  • Kim, Ki-Won (Department of Pharmacology, College of Medicine , Chunbuk National University) ;
  • Kim, Beam-Tae (Department of Chemistry and Research Center of Bioactive Materials, College of Natural Science) ;
  • Lee, Chul-Min (Department of Chemistry and Research Center of Bioactive Materials, College of Natural Science) ;
  • Park, Eun-Young (Department of Pharmacology, College of Medicine , Chunbuk National University) ;
  • Woo, Ran-Sook (Department of Pharmacology, College of Medicine , Chunbuk National University)
  • Published : 2001.08.01
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Abstract

Bioisostere approach has been shown to be useful to augment potency or to modify certain physiological properties of a lead compound. Based upon well documented bioisosterism, an isosteric replacement of benzene ring of 4-hydroxy-2-quinolone compound (L-695902) with a thiophene moiety was carried out to prepare the title compounds, 4-hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (birding assay) for NMDA receptor glycine site.

Keywords

References

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