| L-噻唑烷-4-甲酸的合成及降压活性测定 |
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| 引用本文： | 张洁,代斌,王东,顾承志,刘志勇,李增春.L-噻唑烷-4-甲酸的合成及降压活性测定[J].石河子大学学报,2007,25(3):352-353. |
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| 作者姓名： | 张洁 代斌 王东 顾承志 刘志勇 李增春 |
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| 作者单位： | 石河子大学化学化工学院,新疆石河子,832003;石河子大学医学院,新疆石河子,832003 |
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| 基金项目： | 教育部跨世纪优秀人才培养计划;国家攻关项目创新药物与中药现代化新药博士基金 |
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| 摘 要： | 为寻找新型降压化合物,由L-半胱氨酸盐酸盐及甲醛合成L-噻唑烷-4-甲酸,收率为84.4%,其结构经IR,1H-NMR和元素分析确证。采用经典的二肾一夹法复制肾血管性高血压大鼠(RHR)模型,以卡托普利为对照,通过直接测血压法测定给药后血压变化。初步药理实验结果表明:目标化合物降压作用极显著P<0.01,且表现出作用效果呈剂量依赖性增长。该化合物具有进一步的研究意义。
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| 关 键 词： | L-噻唑烷-4-羧酸 合成 降压作用 |
| 文章编号： | 1007-7383(2007)03-0352-02 |
| 修稿时间： | 2007年3月7日 |
Synthesis and Antihypertensive Activity Study of Thiazolidine-4-carboxylic Acid |
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| ZHANG Jie,DAI Bin,WANG Dong,GU Cheng-zhi,LIU Zhi-yong,LI Zeng-chun.Synthesis and Antihypertensive Activity Study of Thiazolidine-4-carboxylic Acid[J].Journal of Shihezi University(Natural Science),2007,25(3):352-353. |
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| Authors: | ZHANG Jie DAI Bin WANG Dong GU Cheng-zhi LIU Zhi-yong LI Zeng-chun |
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| Abstract: | In order to search for the novel antihypertensive agents,thiazolidine-4-carboxylic acid have been synthesized in 84.4% yields from readily available starting material L-cysteine hydrochloride via condensation reactions.The product was identified by IR,1H-NMR spectra and elemental analysis,and evaluated for their antihypertensive effect of systolic blood pressure(SBP)and diastolic blood pressure(DBP)of the renal hypertensive rats(RHR).Renal hypertensive rats were performed by ligating the left renal artery.The assay results showed that compared with the BP before given drug,thiazolidine-4-carboxylic acid significantly reduced BP of RHR(P<0.01),which is comparable to that of positive drug captopril.The potential compounds increased the antihypertensive effect in a dose dependent manner. |
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| Keywords: | Thiazolidine-4-carboxylic Acid chemical synthesis antihypertensive effect |
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