4-(4-苯基哌嗪-1-基)-3-O-甲基-D-肌醇的制备及镇咳活性 |
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引用本文: | 詹天荣,杨慧娟,范培红,季梅,娄红祥.4-(4-苯基哌嗪-1-基)-3-O-甲基-D-肌醇的制备及镇咳活性[J].中国医药工业杂志,2006,37(12):803-805. |
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作者姓名: | 詹天荣 杨慧娟 范培红 季梅 娄红祥 |
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作者单位: | 1. 山东大学药学院,山东,济南,250012;青岛科技大学化学与分子工程学院,山东,青岛,266042 2. 青岛大学师范学院,山东,青岛,266071 3. 山东大学药学院,山东,济南,250012 |
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摘 要: | 右旋肌醇甲醚经缩酮制化得3-O-甲基-1,2:5,6-二-O-异亚丙基-D-肌醇,经甲磺酰化、水解、与4-苯基哌嗪缩合制得左羟丙哌嗪类似物4-(4-苯基哌嗪-1-基)-3-O-甲基-D-肌醇,总收率38%。镇咳药效实验表明,目标物对致咳小鼠的镇咳作用明显,但不及左羟丙哌嗪。
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关 键 词: | 4-(4-苯基哌嗪-1-基)-3-O-甲基-D-肌醇 左羟丙哌嗪 镇咳活性 制备 |
文章编号: | 1001-8255(2006)12-0803-03 |
收稿时间: | 2006-03-14 |
修稿时间: | 2006-03-14 |
Preparation and Antitussive Activity of 4- (4-Phenylpiperazin- 1-yl) -3-O-methyl-D-inositol |
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Authors: | ZHAN Tian-Rong YANG Hui-Juan FAN Pei-Hong JI Mei LOU Hong-Xiang |
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Institution: | 1. School of Pharmaceutical Sciences, Shandong University, Jinan 250012; 2. College of Chemistry and Molecular Engineering, Qingdao University of Science and Technology, Qingdao 266042; 3. Teachers College of Qingdao University, Qingdao 266071 |
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Abstract: | 4-(4-Phenylpiperazin-1-yl)-3-O-methyl-D-inositol, an analog of levodropropizine was synthesized from pinitol by ketalation, mesylation, hydrolysis and condensation with 4-phenylpiperazine in 38% overall yield. The preliminary antitussive activity was evaluated, and the results showed that the title compound had significant antitussive effect on citric acid induced cough on Winstar rats. |
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Keywords: | 4-(4-phenylpiperazin-1-yl)-3-O-methyl-D-inositol levodropropizine antitussive activity preparation |
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