Chemoenzymatic synthesis and binding affinity of novel (R)- and (S)-3-aminomethyl-1-tetralones, potential atypical antipsychotics

被引：9

作者：

Caro, Y

Torrado, M

Masaguer, CF

Raviña, E

Padín, F

Brea, J

Loza, MI

机构：

[1] Univ Santiago de Compostela, Fac Farm, Drug Res & Dev Grp,Lab Quim Farmaceut, Dept Quim Organ, E-15782 Santiago De Compostela, Spain

[2] Univ Santiago de Compostela, Fac Farm, Dept Farmacol, E-15782 Santiago De Compostela, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

aminomethyltetralones; enzymatic resolution; dopamine receptors; serotonin receptors; antipsychotics;

D O I：

10.1016/j.bmcl.2003.11.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of (R)- and (S)-3-aminomethyl-1-tetralones, conformationally constrained analogues of haloperidol, have been obtained by enzymatic resolution of the corresponding racemic 3-hydroxymethyl-1-tetralones using Pseudomonasfluorescens lipase. Their binding affinities at dopamine D-2 and serotonin 5-HT2A and 5-HT2C receptors were determined showing in some cases an atypical antipsychotic profile with Meltzer's ratio higher than 1.30. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：585 / 589

页数：5

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