| 2-(取代苯乙烯基)吲哚类衍生物的合成及其生物活性 |
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| 引用本文： | 徐莉,徐世平. 2-(取代苯乙烯基)吲哚类衍生物的合成及其生物活性[J]. 药学学报, 2001, 36(2): 100-104 |
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| 作者姓名： | 徐莉 徐世平 |
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| 作者单位： | [1]中国医学科学院、中国协和医科大学药物研究所，北京１０００５０ [2]中国医学科学院、中国协和医科大学药物研究 |
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| 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。
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| 关 键 词： | 吲哚衍生物 Wittig-Horner反应 受体 |
| 收稿时间： | 2000-05-10 |
SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-[(SUBSTITUTED PHENYL)VINYL] INDOLE DERIVATIVES |
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| XU Li,XU Shi-ping. SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-[(SUBSTITUTED PHENYL)VINYL] INDOLE DERIVATIVES[J]. Acta pharmaceutica Sinica, 2001, 36(2): 100-104 |
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| Authors: | XU Li XU Shi-ping |
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| Affiliation: | Institute of Materia Medica, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China. |
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| 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 alpha 2, D2 and H1, and is worth further studying. |
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| Keywords: | Wittig-Horner reaction receptor indole derivatives |
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