Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif

[摘要]：A series of 8 new tetrahydroquinazolinone derivatives was synthesized and evaluated for binding affinity to D-2 and 5-HT2A human receptors; in addition, some properties related to blood-brain barrier penetration were calculated. From the results of these assays, three compounds were selected for further binding tests on D-1, D-3, and 5-HT2C human receptors, which are thought to be involved in schizophrenia. From these data, compound 19b emerged as the most promising candidate based on its good binding affinities for D-1, D-2, and D-3 receptors, high affinity for 5-HT2A, low affinity for 5-HT2C receptors, and a Meltzer's ratio characteristic of an atypical antipsychotic profile. (C) 2009 Elsevier Ltd. All rights reserved.

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