1. Novel non-nucleobase inhibitors of Staphylococcus aureus DNA polymerase IIIC
- Author
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Rose, Yannick, Ciblat, Stéphane, Reddy, Ranga, Belley, Adam C., Dietrich, Evelyne, Lehoux, Dario, McKay, Geoffrey A., Poirier, Hugo, Far, Adel Rafai, and Delorme, Daniel
- Subjects
- *
DNA polymerases , *STAPHYLOCOCCUS aureus , *ANTI-infective agents , *STAPHYLOCOCCUS - Abstract
Abstract: The preparation and biological evaluation of 5-substituted-6-hydroxy-2-(anilino)pyrimidinones as a new class of DNA polymerase IIIC inhibitors, required for the replication of chromosomal DNA in Gram-positive bacteria, are described. These new dGTP competitive inhibitors displayed good levels of in vitro inhibition and antibacterial activity against Staphylococcus aureus. A new class of dATP competitive inhibitors, 6-substituted-2-amino-5-alkyl-pyrimidin-4-ones, whose antibacterial activity was unaffected by serum, were identified. [Copyright &y& Elsevier]
- Published
- 2006
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