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3-甲基-7-氧-9-氟-10-烃氧基(或芳氧基)-2,3-二氢-7H-吡啶[ 1,2,3-de]苯并恶嗪-6-羧酸及其类似物(英) 的合成和抗菌以及抗肿瘤活性

Synthesis, Antibacterial and Antitumor Activity of 3-Me thy1-7-oxo-9-fluoro-10-alkyloxy (or Aryloxy)-2,3-dihydro-7H pyrido[1,2,3-de] [1,4]benzoxazine-6-carboxylic Acids and An alogues

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【作者】 周伟澄; 刘进前; 余爱珍; 陈秀华; 张秀平;

【Author】 Zhou Weicheng, Liu Jinqian, Yu Aizhen, Chen Xiuhua and Zhang Xiuping (Shanghai Institute of Pharmaceutical Industry, Shanghai 200437)

【机构】 上海医药工业研究院!上海; 200437;

【摘要】 合成了3-甲基-7-氧-9-氟-10-烃氧基(或芳氧基)-2,3-二氢-7H-吡啶[1,2,3-de]苯并恶嗪-6-羧酸及其类似物,体外抗菌筛选证明10-烃氧基化合物(尤其是氟乙氧基化合物3d)的抗菌作用明显优于10-羟基化合物3a。体外抗肿瘤试验证明有的化合物对LAX和P388细胞株培养具有中等或较低的细胞毒。

【Abstract】 Some 3-methyl-7-oxo-9-fluoro-10-alkyloxy (or aryloxy)-2, 3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acids and analogues were synthesized. The in vitroantibacterial tests showed that the effect of the 10-alkyloxy compounds (especially the fluoroethyloxycompound 3d) was much better than that of the 10-hydroxy compound 3a. The antitumor test showedthat some target compounds possessed moderate or low cytotoxicity against LAX and P388 in theculture.

【关键词】 氟喹诺酮; 抗菌; 抗肿瘤;
【Key words】 Fluoroquinolones; Antibacterial activity; Antitumor;
  • 【文献出处】 Journal of Chinese Pharmaceutical Sciences ,中国药学(英文版) , 编辑部邮箱 ,1999年01期
  • 【分类号】R914
  • 【被引频次】2
  • 【下载频次】128
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