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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

Zhou Weicheng, Liu Jinqian, Yu Aizhen, Chen Xiuhua, Zhang Xiuping   

  1. Shanghai Institute of Pharmaceutical Industry, Shanghai 200437
  • Received:1997-10-10 Revised:1998-02-16 Online:1999-03-15 Published:1999-03-15

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 vitro antibacterial 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.

Key words: Fluoroquinolones, Antibacterial activity, Antitumor

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