（±）-表喹酰胺和（±）-C（1）-表表喹酰胺的合成及烟碱结合活性

The synthesis and nicotinic binding activity of (+/-)-epiquinamide and (+/-)-C(1)-epiepiquinamide.

作者信息

Kanakubo Akira, Gray Diane, Innocent Neal, Wonnacott Susan, Gallagher Timothy

机构信息

School of Chemistry, University of Bristol, UK.

出版信息

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4648-51. doi: 10.1016/j.bmcl.2006.05.100. Epub 2006 Jun 19.

DOI:10.1016/j.bmcl.2006.05.100

PMID:16784846

Abstract

The synthesis of (+/-)-epiquinamide 1 and (+/-)-C(1)-epiepiquinamide 2 based on the use of a Curtius rearrangement to introduce the C(1) amino residue is reported. In a competition binding assay for [(3)H]epibatidine binding to rat brain membranes neither (+/-)-1 nor (+/-)-2 showed any significant level of nicotinic activity.

摘要

报道了基于使用库尔提斯重排反应引入C(1)氨基残基来合成(±)-表喹酰胺1和(±)-C(1)-表表喹酰胺2的方法。在[(3)H]埃博霉素与大鼠脑膜结合的竞争结合试验中，(±)-1和(±)-2均未显示出任何显著水平的烟碱活性。