Active site directed inhibitors of replication-specific bacterial DNA polymerases

Bioorg Med Chem Lett. 2005 Feb 1;15(3):729-32. doi: 10.1016/j.bmcl.2004.11.016.

Abstract

7-Substituted-N(2)-(3,4-dichlorobenzyl)guanines potently and competitively inhibit DNA polymerases IIIC and IIIE from Gram(+) bacteria. Certain derivatives are also competitive inhibitors of DNA polymerase IIIE from Gram(-) bacteria.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Bacterial Proteins / antagonists & inhibitors*
  • Binding Sites
  • Binding, Competitive
  • DNA Polymerase III / antagonists & inhibitors
  • DNA Replication / drug effects
  • Gram-Negative Bacteria / enzymology
  • Gram-Positive Bacteria / enzymology
  • Guanine / analogs & derivatives*
  • Guanine / chemical synthesis
  • Guanine / pharmacology
  • Humans
  • Kinetics
  • Nucleic Acid Synthesis Inhibitors*
  • Structure-Activity Relationship
  • Uracil / analogs & derivatives*
  • Uracil / chemical synthesis
  • Uracil / pharmacology

Substances

  • Bacterial Proteins
  • Nucleic Acid Synthesis Inhibitors
  • Uracil
  • Guanine
  • DNA Polymerase III