| 抗血吸虫病药鹤草酚类似物的合成 |
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| 引用本文： | 姚润华,马荣生,陈耀清,黄兰孙. 抗血吸虫病药鹤草酚类似物的合成[J]. 药学学报, 1984, 19(3): 228-231 |
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| 作者姓名： | 姚润华 马荣生 陈耀清 黄兰孙 |
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| 作者单位： | 中国医学科学院寄生虫病研究所 上海(姚润华，马荣生，陈耀清)，中国医学科学院寄生虫病研究所 上海(黄兰孙) |
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| 基金项目： | 联合国开发计划总署/世界银行/世界卫生组织热带病培训特别规划的部分支持 |
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| 摘 要： | 鹤草酚(Agrimophol)(Ⅰ)是从植物仙鹤草(Agrimonia pilosa Ledeb)根芽中分离出来的一种驱绦虫有效成分,王根法等发现它有抗血吸虫作用,但减虫率不高,胃肠道反应也较重。鹤草酚是间苯三酚的衍生物,分子中有角甲基,人工合成较复杂。我们企图改变其化学结构,使成为结构简单而又易于制备并有抗血吸虫活性而毒性低于鹤草酚的类似物。文
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| 关 键 词： | 鹤草酚 抗血吸虫病药 间苯三酚衍生物 |
| 收稿时间： | 1982-11-24 |
SYNTHESIS OF ANALOGS OF AGRIMOPHOL |
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| YAO Run-hua,MA Rong-sheng,CHEN Yao-qing and HUANG Lan-sun. SYNTHESIS OF ANALOGS OF AGRIMOPHOL[J]. Acta pharmaceutica Sinica, 1984, 19(3): 228-231 |
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| Authors: | YAO Run-hua MA Rong-sheng CHEN Yao-qing HUANG Lan-sun |
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| Abstract: | Twenty-three monomeric and dimeric acylphloroglucinol derivatives were synthesized for the purpose of finding analogs of agrimophol with higher antischistosomal activity and lower toxicity and more readily prepared as compared with agrimophol. The monomeric acylphloroglucinols were synthesized by acylating the phloroglucinol with appropriate acyl chloride or acid anhydride in the presence of borontrifluoride; the dimeric compounds were prepared by condensation of two molecules of acylphloroglucinols with formaldehyde or methoxymethylacetate. In animal screening tests compounds 1,3,14,19 and 22 exhibited antischistosomal activity. |
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| Keywords: | Agrimophol Antischistosomal agent Phloroglucinols |
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