Literature DB >> 16298129

Novel non-nucleobase inhibitors of Staphylococcus aureus DNA polymerase IIIC.

Yannick Rose1, Stéphane Ciblat, Ranga Reddy, Adam C Belley, Evelyne Dietrich, Dario Lehoux, Geoffrey A McKay, Hugo Poirier, Adel Rafai Far, Daniel Delorme.   

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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Year:  2005        PMID: 16298129     DOI: 10.1016/j.bmcl.2005.11.009

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Architecture and conservation of the bacterial DNA replication machinery, an underexploited drug target.

Authors:  Andrew Robinson; Rebecca J Causer; Nicholas E Dixon
Journal:  Curr Drug Targets       Date:  2012-03       Impact factor: 3.465

Review 2.  DNA replication proteins as potential targets for antimicrobials in drug-resistant bacterial pathogens.

Authors:  Erika van Eijk; Bert Wittekoek; Ed J Kuijper; Wiep Klaas Smits
Journal:  J Antimicrob Chemother       Date:  2017-05-01       Impact factor: 5.790

Review 3.  Targeting DNA Replication and Repair for the Development of Novel Therapeutics against Tuberculosis.

Authors:  Michael A Reiche; Digby F Warner; Valerie Mizrahi
Journal:  Front Mol Biosci       Date:  2017-11-14

4.  Synthesis and bioactivity evaluation of new 6-aryl-5-cyano thiouracils as potential antimicrobial and anticancer agents.

Authors:  Azza Taher Taher; Sahar Mahmoud Abou-Seri
Journal:  Molecules       Date:  2012-08-17       Impact factor: 4.411

  4 in total

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