4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D 4 receptors

…, PD Leeson, R Marwood, S Patel, S Patel…

文献索引：Moore, Kevin W.; Bonner, Katrine; Jones, Elizabeth A.; Emms, Frances; Leeson, Paul D.; Marwood, Rosemary; Patel, Shil; Patel, Smita; Rowley, Michael; Thomas, Steven; Carling, Robert W. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 9 p. 1285 - 1290

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被引用次数: 36

摘要

The syntheses of a number of different N-linked heterocyclic pyrazole replacements based on the structure 1 are described (compounds 3–12) as hD4 ligands. After further optimisation the best compound identified was 13 which has high affinity for hD4 (5.2 nM) and> 300-fold selectivily for hD4 receptors over hD2 and hD3 receptors.