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标题:Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis
时间:2020-10-18 12:24:48
DOI:10.1016/j.bmc.2012.12.011
大小:508 kb
页数:10 PAGES
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目录:
  • Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis
    • 1 Introduction
    • 2 Results and discussion
      • 2.1 Chemistry
      • 2.2 Antimicrobial activity
        • 2.2.1 MIC determination
        • 2.2.2 Inhibition of M. tuberculosis and M. leprae wild-type DNA gyrases
        • 2.2.3 Drug-inducible DNA cleavage by M. leprae gyrase
      • 2.3 General discussion of structure–activity relationships
      • 2.4 Correlation between MICs, IC50s and CC25s
      • 2.5 Conclusions
    • 3 Materials and methods
      • 3.1 Reagents
      • 3.2 In vitro antimicrobial activity
      • 3.3 DNA supercoiling assay
      • 3.4 DNA cleavage assay
      • 3.5 Correlation between MICs, IC50s and CC25s
      • 3.6 Synthesis
        • 3.6.1 General chemistry methods
        • 3.6.2 Ethyl 1-cyclopropyl-7-(3'-(ethoxycarbonyl)
        • 3.6.3 Ethyl 1-cyclopropyl-7-(3'-(ethoxycarbonyl)
        • 3.6.4 General procedure for the synthesis of compounds (1–6)
          • 3.6.4.1 1-Cyclopropyl-7-(3'-((diethylcarbamoylox
          • 3.6.4.2 1-Cyclopropyl-7-(3'-((diethylcarbamoylox
          • 3.6.4.3 7-(3'-((Butylcarbamoyloxy)methyl)piperaz
          • 3.6.4.4 7-(3'-((Butylcarbamoyloxy)methyl)piperaz
          • 3.6.4.5 1-Cyclopropyl-7-(3'-ethoxycarbonylpipera
          • 3.6.4.6 1-Cyclopropyl-7-(3'-ethylcarbonylpiperaz
        • 3.6.5 General procedure for the synthesis of compounds (7–10)
          • 3.6.5.1 7-(3'-Carboxypiperazin-1-yl)-1-cycloprop
          • 3.6.5.2 1-Cyclopropyl-7-(3'-carboxypiperazin-1-y
          • 3.6.5.3 1-Cyclopropyl-7-(3'-carboxy-4'-ethylpipe
          • 3.6.5.4 1-Cyclopropyl-7-(3'-carboxy-4'-ethylpipe
    • Acknowledgements
    • References and notes

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