王晓莉, 徐鸣夏, 邓力, 周国川, 郑虎. 3-苯基-4(1H)喹啉酮羟基衍生物的合成及其抗骨质疏松活性J. 药学学报, 2002, 37(12): 938-941.
引用本文: 王晓莉, 徐鸣夏, 邓力, 周国川, 郑虎. 3-苯基-4(1H)喹啉酮羟基衍生物的合成及其抗骨质疏松活性J. 药学学报, 2002, 37(12): 938-941.
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WANG Xiao-li, XU Ming-xia, DENG Li, ZHOU Guo-chuan, ZHENG Hu. SYNTHESIS AND ANTIOSTEOPOROSIS ACTIVITY OF 3-PHENYL-4(1H) QUINOLINONE DERIVATIVESJ. Acta Pharmaceutica Sinica, 2002, 37(12): 938-941.
Citation: WANG Xiao-li, XU Ming-xia, DENG Li, ZHOU Guo-chuan, ZHENG Hu. SYNTHESIS AND ANTIOSTEOPOROSIS ACTIVITY OF 3-PHENYL-4(1H) QUINOLINONE DERIVATIVESJ. Acta Pharmaceutica Sinica, 2002, 37(12): 938-941.
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3-苯基-4(1H)喹啉酮羟基衍生物的合成及其抗骨质疏松活性

SYNTHESIS AND ANTIOSTEOPOROSIS ACTIVITY OF 3-PHENYL-4(1H) QUINOLINONE DERIVATIVES

    摘要
  • 摘要: 目的设计并合成7-羟基-3-(取代)苯基-4(1H)喹啉酮化合物及其相应的5-羟基-3-(取代)苯基-4(1H)喹啉酮化合物并考察其抗骨质疏松活性。方法以间氨基酚为原料,选择改良的Gould-Jacobs反应路线同时合成7-羟基-3-(取代)苯基-4(1H)喹啉酮4个(A1～4)及其相应的5-羟基-3-(取代)苯基-4(1H)喹啉酮4个(B1～4),通过骨细胞筛选实验以及羟磷灰石吸附实验分别考察其促骨形成作用和趋骨性。结果共合成了新化合物8个(A1～4,B1～4),其结构经IR,MS,1HNMR和元素分析确证。骨细胞筛选实验结果表明,B3有促骨形成作用,但作用弱于芒柄花黄素;羟磷灰石吸附实验结果表明,羟磷灰石对B1,B2和B4有一定的吸附,其中对B1和B2的吸附作用强于四环素。结论 5-羟基-3-(取代)苯基-4(1H)喹啉酮化合物有促骨形成作用并具有一定的趋骨活性。

     

    Abstract: AIMTo design and synthesize 7-hydroxy-3-(substituted) phenyl-4(1H) quinolinone and 5-hydroxy-3-(substituted) phenyl-4(1H) quinolinone and to study the antiosteoporosis activity of these compounds. METHODSThe compounds of 7-hydroxy and 5-hydroxy were prepared simultaneously by improved Gould-Jacobs reaction and resorcin was used as starting material. Eight compounds (A1～4, B1～4) were synthesized and their chemical structures were determined by IR, MS, 1HNMR and elemental analysis. Their osteoplastic activity was evaluated by the absorptive test to Ca2+ of hydroxyapatite crystal. RESULTSCompounds (A1～4,B1～4) are new compounds. Compounds B1 and B2 showed antiosteoporosis activities and was stronger than the control drug of tetracycline. CONCLUSIONCompounds B1 and B2 are worthy to be intensively studied.

     

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