Pyrrolopyrimidine inhibitors of DNA gyrase B (GyrB) and topoisomerase IV (ParE). Part I: Structure guided discovery and optimization of dual targeting agents with potent, broad-spectrum enzymatic activity.

@article{Tari2013PyrrolopyrimidineIO,
  title={Pyrrolopyrimidine inhibitors of DNA gyrase B (GyrB) and topoisomerase IV (ParE). Part I: Structure guided discovery and optimization of dual targeting agents with potent, broad-spectrum enzymatic activity.},
  author={Leslie W. Tari and Michael Trzoss and Daniel C. Bensen and Xiaoming Li and Zhiyong Chen and Thanh Thu Lam and Junhu Zhang and Christopher J Creighton and Mark L. Cunningham and Bryan P. Kwan and Mark A Stidham and Karen Joy Shaw and Felice C. Lightstone and Sergio E. Wong and Toan B. Nguyen and Jay C. Nix and John E. Finn},
  journal={Bioorganic & medicinal chemistry letters},
  year={2013},
  volume={23 5},
  pages={1529-36}
}
The bacterial topoisomerases DNA gyrase (GyrB) and topoisomerase IV (ParE) are essential enzymes that control the topological state of DNA during replication. The high degree of conservation in the ATP-binding pockets of these enzymes make them appealing targets for broad-spectrum inhibitor development. A pyrrolopyrimidine scaffold was identified from a pharmacophore-based fragment screen with optimization potential. Structural characterization of inhibitor complexes conducted using selected… CONTINUE READING

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