【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。更多还原

【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.更多还原