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为寻找高选择性的α1-受体拮抗剂,该文分别以3-羟基二苯甲酮和4-甲氧基苯酚为原料,在碱性条件下与3-氯-1,2-环氧丙烷(Ⅱ)发生取代反应,得到3-取代苯氧基-1,2-环氧丙烷(Ⅲ),再经芳基哌嗪开环合成了7个3-苯甲酰基苯氧基取代和对甲氧基苯氧基取代的哌嗪-2-丙醇类化合物(Ⅴa~Ⅴg),其结构经1HNMR、MS、IR和元素分析确证。采用大鼠离体肛尾肌张力实验对目标化合物的α1-受体拮抗活性进行了测试,结果显示,这些化合物均具有较好的α1-受体拮抗活性(pA2>6),其中化合物(Ⅴg)活性最强(pA2=8.13±0.25)。
In order to search for highly selective α1-receptor antagonists, 3-hydroxybenzophenone and 4-methoxyphenol were used as starting materials respectively and reacted with 3-chloro-1,2-epoxy Propane (Ⅱ) substitution reaction to give 3-substituted phenoxy-1,2-propylene oxide (Ⅲ), followed by aryl piperazine ring opened seven 7 - benzoyl phenoxy substitution and Methoxyphenoxy substituted piperazine-2-propanol compounds (Va ~ Vg) were synthesized and their structures were confirmed by 1HNMR, MS, IR and elemental analysis. The α1-adrenoceptor antagonistic activity of the target compounds was tested using rat tail muscle tone test. The results showed that all these compounds have good α1-receptor antagonistic activity (pA2> 6), and the compounds (Ⅴg ) Was the most active (pA2 = 8.13 ± 0.25).