杨玉社, 嵇汝运, 陈凯先, 丁健. 左旋氧氟沙星类似物的合成及其抗菌抗肿瘤活性研究J. 药学学报, 1999, 34(2): 119-124.
引用本文: 杨玉社, 嵇汝运, 陈凯先, 丁健. 左旋氧氟沙星类似物的合成及其抗菌抗肿瘤活性研究J. 药学学报, 1999, 34(2): 119-124.
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Yang Yushe, Ji Ruyun, Chen Kaixian , Ding Jian, . STUDIES ON SYNTHESIS ANTIBACTERIAL AND ANTITUMOR ACTIVITY OF (S)-(-)-OFLOXACIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1999, 34(2): 119-124.
Citation: Yang Yushe, Ji Ruyun, Chen Kaixian , Ding Jian, . STUDIES ON SYNTHESIS ANTIBACTERIAL AND ANTITUMOR ACTIVITY OF (S)-(-)-OFLOXACIN ANALOGUESJ. Acta Pharmaceutica Sinica, 1999, 34(2): 119-124.
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左旋氧氟沙星类似物的合成及其抗菌抗肿瘤活性研究

STUDIES ON SYNTHESIS ANTIBACTERIAL AND ANTITUMOR ACTIVITY OF (S)-(-)-OFLOXACIN ANALOGUES

    摘要
  • 摘要: 目的：设计合成有抗菌抗肿瘤活性的喹诺酮药物。方法和结果：根据推理药物设计原理，设计并合成了16个新型抗菌抗肿瘤喹诺酮类化合物，并研究其构效关系。结论：用9株细菌及4株肿瘤细胞评价了它们的体外抗菌活性(MIC值)及抗肿瘤活性(抑瘤率%)。其中，化合物16～20有较好的抗肿瘤及抗菌活性。

     

    Abstract: AIM: To design and prepare quinolone compounds with antibacterial and antitumor activities. METHODS AND RESULTS: According to rational drug design principle, a series of novel analogues of (S)-(-)-ofloxacin has been prepared and the influences on structure-activity relationships was also discussed. CONCLUSION: Their in vitro antitumor and antibacterial activities were evaluated. The results showed that compound 16～20 have good antitumor and antibacterial activities.

     

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