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Pyridine-3-carboxamide-6-yl-ureas as novel inhibitors of bacterial DNA gyrase: structure based design, synthesis, SAR and antimicrobial activity

By Lloyd Czaplewski, Aug 21 2015 12:36PM

Yule IA, Czaplewski LG, Pommier S, Davies DT, Narramore SK, Fishwick CW.

Eur J Med Chem. 2014 Oct 30;86:31-8. doi: 10.1016/j.ejmech.2014.08.025. Epub 2014 Aug 7.


The development of antibacterial drugs based on novel chemotypes is essential to the future management of serious drug resistant infections. We herein report the design, synthesis and SAR of a novel series of N-ethylurea inhibitors based on a pyridine-3-carboxamide scaffold targeting the ATPase sub-unit of DNA gyrase. Consideration of structural aspects of the GyrB ATPase site has aided the development of this series resulting in derivatives that demonstrate excellent enzyme inhibitory activity coupled to potent Gram positive antibacterial efficacy.

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