Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379247 | Bioorganic & Medicinal Chemistry Letters | 2006 | 6 Pages |
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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Authors
Yannick Rose, Stéphane Ciblat, Ranga Reddy, Adam C. Belley, Evelyne Dietrich, Dario Lehoux, Geoffrey A. McKay, Hugo Poirier, Adel Rafai Far, Daniel Delorme,