高级检索
张江波, 陈国华, 罗小川, 吴斐华. 吲哚啉类α1-肾上腺素受体拮抗剂的合成及生物活性[J]. 中国药科大学学报, 2009, 40(3): 200-204.
引用本文: 张江波, 陈国华, 罗小川, 吴斐华. 吲哚啉类α1-肾上腺素受体拮抗剂的合成及生物活性[J]. 中国药科大学学报, 2009, 40(3): 200-204.
shu
ZHANG Jiang-bo, CHEN Guo-hua, LUO Xiao-chuan, WU Fei-hua. Synthesis and biological activity of indoline compounds as α1-AR antagonist[J]. Journal of China Pharmaceutical University, 2009, 40(3): 200-204.
Citation: ZHANG Jiang-bo, CHEN Guo-hua, LUO Xiao-chuan, WU Fei-hua. Synthesis and biological activity of indoline compounds as α1-AR antagonist[J]. Journal of China Pharmaceutical University, 2009, 40(3): 200-204.
shu

吲哚啉类α1-肾上腺素受体拮抗剂的合成及生物活性

Synthesis and biological activity of indoline compounds as α1-AR antagonist

    摘要
  • 摘要: 目的 ： 寻找新的α1-肾上腺素受体（α1-AR）拮抗剂。 方法 ： 以西洛多辛为先导化合物，保留其药效基团吲哚啉母核，依据拼合原理，引入取代苯氧基烷基哌嗪基团，设计合成了12个5-［2-［4-(取代苯氧基烷基)-1-哌嗪基］丙基］吲哚啉类化合物。 结果 ： 目标化合物结构经元素分析、红外光谱、质谱和核磁共振氢谱确证，初步药理实验结果表明，6个目标化合物的拮抗参数pA2值大于7.50，具有较好的α1-AR拮抗活性。 结论 ： 5-［2-［4-(取代苯氧基烷基)-1-哌嗪基］丙基］吲哚啉类化合物是一类新型的具有潜在价值的α1-AR拮抗剂。

     

    Abstract: Aim ：To search for novel α1-adrenoceptor(α1-AR) antagonists. Methods ：On the basis of hybridization principle with silodosin as the lead compound，twelve 5-［2-［4-［(substituted phenoxy)alkyl］piperazin-1-yl］propyl］indoline compounds were designed and synthesized by maintaining indoline while incorporating the 1-［(substituted phenoxy)alkyl］piperazine group. Results ：The structures of synthesized target compounds were confirmed by the elemental analysis，IR，ESI-MS and 1H NMR.Preliminary pharmacological test showed that pA2 values of six target compounds were greater than 7.50，which suggested that the compounds possessed considerable α1-AR antagonic activity. Conclusion ：5-［2-［4-［(substituted phenoxy)alkyl］piperazin-1-yl］propyl］indoline compounds is potentially a new candidate for α1-AR antagonist.

     

    • HTML全文
    • 参考文献(0)
    • 相关文章
    • 施引文献
  • 资源附件(0)

/

返回文章
返回

访问量：