【摘要】 根据拼合原理,以1-乙酰基吲哚啉为起始原料,设计合成了1-乙酰基-5-{2-[4-(取代苯氧基乙基)-1-哌嗪基]烷基}吲哚啉和1-乙酰基-5-[2-(4-取代苯基-1-哌嗪基)烷基]吲哚啉两类化合物,所有目标化合物结构均经核磁共振氢谱、元素分析、红外光谱及质谱确证.初步生物活性测试结果表明,所有目标化合物均具有一定的α1-AR拮抗活性.更多还原

【Abstract】 As benign prostate hyperplasia(BPH) is a common disease in elderly men,it is urgent to find new α1-adrenoceptor(AR) antagonists,the first choice for the therapy of BPH.On the basis of hybridization principle with 1-acetylindoline as the starting compound,two series of indoline derivatives 1-acetyl-5-{2-[4-(substituted phenoxy)ethyl]piperazin-1-yl}alkyl indoline and 1-acetyl-5-{2-[4-(substituted phenyl)piperazin-1-yl]alkyl} indoline were designed and synthesized.The structures of the target compounds were confirmed by 1H NMR,elemental analysis,IR and MS.Preliminary pharmacological test show all the target compounds exhibit certain antagonism of α1-AR.Compounds 9h and 12l perform better than piperazine,and are worth of further research.更多还原