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4-(4-苯基哌嗪-1-基)-3-O-甲基-D-肌醇的制备及镇咳活性
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.
作者姓名:詹天荣  杨慧娟  范培红  季梅  娄红祥
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
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。

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
Authors:ZHAN Tian-Rong  YANG Hui-Juan  FAN Pei-Hong  JI Mei  LOU Hong-Xiang
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
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.
Keywords:4-(4-phenylpiperazin-1-yl)-3-O-methyl-D-inositol  levodropropizine  antitussive activity  preparation
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