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] pyrimidines15. The resulting bioisosteric compounds15 were evaluated for their antagonistic activity (binding assay) for NMDA receptor glycine site.
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Hwang, KJ., Lee, TS., Kim, KW. et al. 4-Hydroxy-6-Oxo-6,7-Dihydro-Thieno[2,3-b] pyrimidine derivatives: Synthesis and their biological evaluation for the glycine site acting on theN-Methyl-D-aspartate (NMDA) receptor. Arch Pharm Res 24, 270–275 (2001). https://doi.org/10.1007/BF02975090
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DOI: https://doi.org/10.1007/BF02975090