新型芳基哌嗪模型的合成与构效关系。3.1 2-[ω-(4-芳基哌嗪-1-基)烷基]全氢吡咯并[1,2-c]咪唑和全氢咪唑并[1,5-a]吡啶：末端酰胺片段对5-HT1A亲和力/选择性影响的研究。

Synthesis and structure-activity relationships of a new model of arylpiperazines. 3.1 2-[omega-(4-arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: study of the influence of the terminal amide fragment on 5-HT1A affinity/selectivity.

作者信息

López-Rodríguez M L, Morcillo M J, Fernández E, Porras E, Murcia M, Sanz A M, Orensanz L

机构信息

Departamento de Química Orgánica I, Facultad de Ciencias Químicas, Universidad Complutense, Madrid, Spain.

出版信息

J Med Chem. 1997 Aug 1;40(16):2653-6. doi: 10.1021/jm970216k.

DOI:10.1021/jm970216k

Abstract

A series of new arylpiperazine derivatives 2, which are devoid of the terminal amide fragment present in related 5-HT1A ligands, was prepared and evaluated for affinity at 5-HT1A and alpha 1 receptors. All the compounds 2 demonstrated high affinity for the 5-HT1A receptor and moderate affinity for alpha 1 receptor binding sites. Structure-activity relationship (SAR) studies suggest that there is influence of electronic factors on the no-pharmacophoric part of the alpha 1 receptor site. However there is no influence of electronic interactions on the stabilization of the 5-HT1A receptor-ligand complex.

摘要

制备了一系列新的芳基哌嗪衍生物2，这些衍生物没有相关5-HT1A配体中存在的末端酰胺片段，并对其与5-HT1A和α1受体的亲和力进行了评估。所有化合物2对5-HT1A受体表现出高亲和力，对α1受体结合位点表现出中等亲和力。构效关系（SAR）研究表明，电子因素对α1受体位点的非药效基团部分有影响。然而，电子相互作用对5-HT1A受体-配体复合物的稳定性没有影响。

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