摘要
目的设计合成苯乙胺类α1-肾上腺素受体(α1-AR)拮抗剂,并研究它们对大鼠肛尾肌收缩功能的影响。方法以DDPH为先导化合物设计合成了11个新化合物,以2,6-二甲基苯酚为原料经多步反应得中间体卤代苯氧丙酮,再经还原胺化得目标物。运用大鼠肛尾肌收缩功能实验测定目标物的拮抗活性。结果共合成了11个目的物,其结构经IR、HRMS1、H-NMR确证。结论生物活性测试显示大部分目标化合物均具有一定的α1-AR拮抗活性,化合物Ⅲk拮抗作用和DDPH接近。
Aim To study the blocking activity of 2, 4-dimethoxyphenylethylamine analogues as α1-adrenocepter（α1-AR） antagonist. Methods Based on the biological activity of DDPH, 11 analogues of 2, 4- dimethoxyphylethylamines were designed and prepared. The target compounds were synthesized from 2, 6- dimetbylphenol. Their structures were confirmed by HRMS, ^1H-NMR, IR spectra. Their bioaetivities were also tested. Results The result indicated that most the target compounds exhibited well in blocking α1- adrenoceptor. Conclusion The preliminary bioassay indicates that compound Ⅲ k functions well in blocking α1-adrenoceptor.
出处
《中国药物化学杂志》
CAS
CSCD
2008年第6期401-405,共5页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金项目(30600776)
国家高技术研究发展计划项目(863项目
2002AA2Z3118)
