Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases

被引：19

作者：

Linz, Sabine ^{[1
]}

Mueller, Joerg ^{[1
]}

Huebner, Harald ^{[1
]}

Gmeiner, Peter ^{[1
]}

Troschuetz, Reinhard ^{[1
]}

机构：

[1] Univ Erlangen Nurnberg, Lehrstuhl Pharmazeut Chem, Dept Chem & Pharm, D-91052 Erlangen, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 13期

关键词：

Mannich bases; Dopamine; Heterocyclic compounds; D4; receptor; HIGH-AFFINITY; DERIVATIVES; PYRIMIDINES; AGONISTS;

D O I：

10.1016/j.bmc.2009.05.015

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of phenylpiperazine-methyl-substituted 1H-pyrrolo[2,3-c] pyridine, imidazo[1,2-c]-, pyrrolo[2,3-d]- and pyrrolo[3,2-d] pyrimidines were prepared as selective dopamine D4-ligands. The pyrrolo[2,3-d] pyrimidine derivatives 12d (K-i = 1,9 nM) and 34d (K-i = 2,4 nM) as well as the pyrrolo[3,2-d] pyrimidine Mannich base 49f (K-i = 2,8 nM) showed high dopamine D4 receptor activity superior to the atypical antipsychotic agent clozapine. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4448 / 4458

页数：11

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