Novel non-nucleobase inhibitors of Staphylococcus aureus DNA polymerase IIIC |
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Authors: | Rose Yannick Ciblat Stéphane Reddy Ranga Belley Adam C Dietrich Evelyne Lehoux Dario McKay Geoffrey A Poirier Hugo Far Adel Rafai Delorme Daniel |
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Institution: | Targanta Therapeutics Inc., 7170 Frederick-Banting, 2nd Floor, Montréal, Québec, Canada H4S 2A1. yrose@targanta.com |
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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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