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  • Title: Novel non-nucleobase inhibitors of Staphylococcus aureus DNA polymerase IIIC.
    Author: Rose Y, Ciblat S, Reddy R, Belley AC, Dietrich E, Lehoux D, McKay GA, Poirier H, Far AR, Delorme D.
    Journal: Bioorg Med Chem Lett; 2006 Feb 15; 16(4):891-6. PubMed ID: 16298129.
    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.
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