Active site directed inhibitors of replication-specific bacterial DNA polymerases

[Display omitted] 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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-02, Vol.15 (3), p.729-732
Main Authors: Wright, George E., Brown, Neal C., Xu, Wei-Chu, Long, Zheng-yu, Zhi, Chengxin, Gambino, Joseph J., Barnes, Marjorie H., Butler, Michelle M.
Format: Article
Language:English
Subjects:
Antibacterial
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Bacterial Proteins - antagonists & inhibitors
Binding Sites
Binding, Competitive
Biological and medical sciences
Broad spectrum
Competitive inhibitors
DNA polymerase
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
Medical sciences
Nucleic Acid Synthesis Inhibitors
Pharmacology. Drug treatments
Replication
Structure-Activity Relationship
Uracil - analogs & derivatives
Uracil - chemical synthesis
Uracil - pharmacology
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Description
Summary:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.11.016