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苯并二氢吡喃腙衍生物的合成及其初步药理活性
引用本文:熊晓云,梅其炳,邹永. 苯并二氢吡喃腙衍生物的合成及其初步药理活性[J]. 中国药物化学杂志, 2000, 10(4): 258-261
作者姓名:熊晓云  梅其炳  邹永
作者单位:第四军医大学药理教研室!西安710032(熊晓云,梅其炳,甘洪全,招明高,赵德化),中国科学院广州化学研究所!广州510650(邹永)
摘    要:为进一步筛选活性更强、副作用更小的抗绝经后骨质疏松症药物 ,在综合考察雷洛昔芬和异丙氧基异黄酮的基础上 ,设计合成一系列苯并二氢吡喃腙化合物 .化合物的结构均经波谱鉴定 ,并通过研究其对幼年小鼠子宫增重和血碱性磷酸酶活性的影响 ,初步考察化合物的药理活性 .结果表明 ,XY990 2具有较弱的雌激素受体激动作用和一定的雌激素受体拮抗作用 ,并有助于成骨细胞增殖 ,对治疗骨质疏松症是有利的 .

关 键 词:苯并二氢吡喃腙  异丙氧基异黄酮  雷洛昔芬  绝经后骨质疏松症
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Synthesisof 2,3-dihydro-7-methoxy-4H-1-benzopyran-4-hydrazoneDerivatives and Preliminary Evaluations of Their Pharmacological Activities
Xiong Xiaoyun,Mei Qibing,Zou Yong ,Gan Hongquan,Zhao Minggao,Zhao Dehua. Synthesisof 2,3-dihydro-7-methoxy-4H-1-benzopyran-4-hydrazoneDerivatives and Preliminary Evaluations of Their Pharmacological Activities[J]. Chinese Journal of Medicinal Chemistry, 2000, 10(4): 258-261
Authors:Xiong Xiaoyun  Mei Qibing  Zou Yong   Gan Hongquan  Zhao Minggao  Zhao Dehua
Affiliation:Xiong Xiaoyun,Mei Qibing,Zou Yong 1,Gan Hongquan,Zhao Minggao,Zhao Dehua
Abstract:In order to screen out optimal drugs against postmenopausal osteoporosis,a series of 2,3 dihydro 7 methoxy 4 H 1 benzopyran 4 hydrazone derivatives was designed and synthesized in view of comprehensive observations of raloxifene and ipriflvone.Their structures were determined by spectrums and their preliminary pharmacological activities were evaluated by observing their effects on the uterus weight and blood ALP of young mice.It is indicated that XY9902 is a weak estrogen receptor agonist and partly estrogen receptor antagonist.Additionly XY9902 is helpful to proliferation of osteoblast,which benefits osteoporosis.
Keywords:dihydro 7 methoxy 4 H 1 benzopyran 4 hydrazone  raloxifene  ipriflvone  postosteoporosis
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