Author/Authors :
Yannick Rose، نويسنده , , Stéphane Ciblat، نويسنده , , S. Ranga Reddy and P. Manikyamba، نويسنده , , Adam C. Belley، نويسنده , , Evelyne Dietrich، نويسنده , , Dario Lehoux، نويسنده , , Geoffrey A. McKay، نويسنده , , Hugo Poirier، نويسنده , , Adel Rafai Far، نويسنده , , Daniel Delorme، نويسنده ,
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.
Keywords :
antimicrobial , Antibacterial , DNA polymerase IIIC , In Vivo , Protein binding
