2-(取代苯乙烯基)吲哚类衍生物的合成及其生物活性

SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-(SUBSTITUTED PHENYL)VINYL INDOLE DERIVATIVES

摘要: 目的　寻找有生物活性的吲哚类化合物。方法　用还原、氧化和Witting反应设计合成了21个2-(取代苯基乙烯基)吲哚化合物，用¹HNMR，MS和元素分析确证其结构，并对其进行了体外筛选实验。结果　这些化合物均为新化合物。结论　6个化合物(3，9，11，13，18和20)对组胺1受体、多巴胺2受体和肾上腺素α-2受体有相当的抑制作用，值得进一步研究。

Abstract: AIM　To synthesize derivatives of 2-substituted phenyl)vinyl indole and find compounds with biological activities by screening in vitro. METHODS　Twenty-one compounds of 2-(substituted phenyl)vinyl indole were synthesized by reduction, oxidation and Witting reaction. MS, ¹HNMR and elemental analysis were used to determine the structures of the new compounds. RESULTS　These compounds are new ones. CONCLUSION　Six compounds (3,9,11,13,18 and 20) showed effects on some different receptors, such as alpha2, D2 and H1, and is worth further studying.