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标题:Design, synthesis and activity against Toxoplasma gondii, Plasmodium spp., and Mycobacterium tuberculosis of new 6-fluoroquinolones
时间:2020-10-18 12:42:17
DOI:10.1016/j.ejmech.2006.07.003
大小:631 kb
页数:17 PAGES
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目录:
  • Design, synthesis and activity against Toxoplasma gondii, Plasmodium spp., and Mycobacterium tuberculosis of new 6-fluoroquinolones
    • Introduction
    • Chemistry
    • Pharmacology
    • Results and discussion
      • Design rationale
      • Anti-T. gondii activity
      • Anti-P. falciparum and P. yoelii yoelii activities
      • SAR studies
      • Antibacterial activity against M. tuberculosis and SAR study
    • Conclusion
    • Materials and methods
      • Design of quinolones
      • Chemistry
        • General methods, reagents and starting materials
        • Synthesis of alpha-enamino-beta-ketoesters
          • Ethyl alpha(E)-[(diethylamino)methylene]-2,4,5-trifluoro-3-methoxy-beta-oxo-benzenepropanoate, 18a
          • Ethyl alpha(E)-[(diethylamino)methylene]-3-ethyl-2,4,5-trifluoro-beta-oxo-benzenepropanoate, 18c
        • Synthesis of ethyl 6,7-difluoro-8-substituted quinoline-carboxylates (cyclization step)
          • Ethyl 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline-carboxylate, 20a1
          • Ethyl 1-(2,4-difluorophenyl)-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline-carboxylate, 20a2
          • Ethyl 1-cyclopropyl-8-ethyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylate, 20c1
          • Ethyl 8-ethyl-1-(2,4-difluorophenyl)-6,7-difluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylate, 20c2
        • Synthesis of boron complexes
          • (1-Cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline-carboxylato-O3,O4)difluoro-boron, 21a1
          • (1-(2,4-Difluorophenyl)-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylato-O3,O4)difluoro-boron, 21a2
          • (1-Cyclopropyl-8-ethyl-6,7-difluoro-1,4-dihydro-4-oxo-3-quinoline-carboxylato-O3,O4)difluoro-boron, 21c1
          • (8-Ethyl-1-(2,4-difluorophenyl)-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylato-O3,O4) difluoro-boron, 21c2
        • Synthesis of 7-amino-derived-6-fluoro-8-methoxy-quinolinecarboxylic acids, 1-4
          • 7-[(1alpha,5alpha,6alpha)-6-Amino-3-azabicyclo[3.1.0]hex-3-yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, 1
            • 1-Cyclopropyl-7-[(1alpha,5alpha,6alpha)-6-[[(1,1-dimethylethoxy)carbonyl]amino]-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, 1-Boc
            • Synthesis of 1 (as its 2.6 TFA salt)
          • 7-[(1alpha,5alpha,6alpha)-6-(Aminomethyl)-3-azabicyclo[3.1.0]hex-3-yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, 2
            • 1-Cyclopropyl-7-[(1alpha,5alpha,6alpha)-6-[[[(1,1-dimethylethoxy)carbonyl]amino]-methyl]-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, 2-Boc
            • Synthesis of 2 (as its 0.6 TFA salt)
          • 7-[(1alpha,5alpha,6alpha)-6-Amino-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluoro-phenyl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, 3
            • 1-(2,4-Difluorophenyl)-7-[(1alpha,5alpha,6alpha)-6-[[(1,1-dimethylethoxy)carbonyl]-amino]-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, 3-Boc
            • Synthesis of 3 (as its 1.6 TFA salt)
          • 7-[(1alpha,5alpha,6alpha)-6-(Aminomethyl)-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, 4
            • 1-(2,4-Difluorophenyl)-7-[(1alpha,5alpha,6alpha)-6-[[[(1,1-dimethylethoxy)carbonyl]-amino]methyl]-3-azabicyclo[3.1.0]hex-3-yl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid, 4-Boc
            • Synthesis of 4 (as its 1.2 TFA salt)
      • Biological assays
        • In vitro antiparasitical activities
          • Anti-T. gondii activity
          • Anti-P. falciparum activity
          • Anti-P. yoelii yoelii activity
        • Inhibitory activity against DNA gyrase of M. tuberculosis
        • In vitro antibacterial activity against M. tuberculosis - determination of MICs
    • Acknowledgements
    • References

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