Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.

@article{Charifson2008NovelDB,
  title={Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.},
  author={Paul S. Charifson and A. Grillot and Trudy H. Grossman and Jonathan D. Parsons and Michael C. Badia and Steve Bellon and David Deininger and Joseph Eugene Drumm and Christian H Gross and Arnaud LeTiran and Yusheng Liao and Nagraj Mani and David P Nicolau and Emanuele Perola and Steven M. Ronkin and Dean E. Shannon and Lora L Swenson and Qing Tao Tang and Pamela R. Tessier and Ski-Kai Tian and Martin Trudeau and Tiansheng Wang and Yunyi Wei and Hong Yun Zhang and Dean Stamos},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 17},
  pages={
          5243-63
        }
}
  • Paul S. Charifson, A. Grillot, +22 authors Dean Stamos
  • Published in
    Journal of medicinal…
    2008
  • Chemistry, Medicine
  • The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all currently used classes of antibiotics. Bacterial DNA gyrase and topoisomerase IV are well-characterized clinically validated targets of the fluoroquinolone antibiotics which exert their antibacterial activity through inhibition of the catalytic subunits. Inhibition of these targets through interaction with their ATP sites has been less… CONTINUE READING

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