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- Title
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.
- Authors
Hwang, Ki-Jun; Lee, Tae-Suk; Kim, Ki-Won; Kim, Beom-Tae; Lee, Chul-Min; Park, Eun-Young; Woo, Ran-Sook
- 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 (binding assay) for NMDA receptor glycine site.
- Publication
Archives of Pharmacal Research, 2001, Vol 24, Issue 4, p270
- ISSN
0253-6269
- Publication type
Article
- DOI
10.1007/BF02975090