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目的 :研究 5 甲氧基色胺苯基哌嗪衍生物的合成及其α1 受体拮抗活性。方法 :由取代苯胺通过环合、取代和胺解等反应合成目的物 ;测定目的物体外α1 受体拮抗活性。结果 :合成了 14个新化合物 ,其结构经IR ,1HNMR和ESI MS质谱确证 ;化合物WBⅠ 2、WBⅠ 3、WBⅠ 4、WBⅠ 8、WBⅠ 9和WBⅠ 14对大鼠肛尾肌动脉环有一定的抑制作用 (抑制率大于 5 0 % )。结论 :初步生物活性测试表明 ,所合成的化合物活性 (pA2 )低于阳性对照药哌唑嗪。
Objective: To study the synthesis of 5-methoxytryptophan phenyl piperazine derivatives and their α1 receptor antagonistic activity. Methods: The target compounds were synthesized by the reaction of substituted anilines through cyclization, substitution and amidolytic reaction. The α1 receptor antagonistic activities of the target compounds were determined. Results: Fourteen new compounds were synthesized and their structures were confirmed by IR, 1HNMR and ESI MS. The compounds WBI 2, WBI 3, WBI 4, WBI 8, WBI 9 and WBI 14 had certain Inhibition (inhibition rate greater than 50%). Conclusion: The preliminary bioassay showed that the activity of the synthesized compound (pA2) was lower than that of the positive control prazosin.