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KMID : 0043320010240040270
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Archives of Pharmacal Research
2001 Volume.24 No. 4 p.270 ~ p.275
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4-Hydroxr-6-Oxo-6,7-Dihydro-Thieno[2,3-b] Pyrimidine Deriyatives : Synthesis and Their Biological Ewaluation for the Glycine Site Acting on the N-Methyl-D-Aspartate (NMDA) Recep tor
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Hwnag KJ
Lee TS/Kim KW/Kim BT/Lee CM/Park EY/Woo RS
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Abstract
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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, a n 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-bl pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (binding assay) for NMDA receptor glycine site.
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