Abstract
High throughput screening led to the discovery of a novel series of quinazolin-2-ylamino-quinazolin-4-ols as a new class of DNA polymerase III inhibitors. The inhibition of chromosomal DNA replication results in bacterial cell death. The synthesis, structure-activity relationships and functional activity are described.
MeSH terms
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Cell Death
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Chemistry, Pharmaceutical / methods*
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DNA / chemistry
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DNA Polymerase III / antagonists & inhibitors*
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DNA Polymerase III / chemistry*
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Drug Design
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Drug Evaluation, Preclinical
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Humans
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Models, Biological
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Models, Chemical
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Molecular Structure
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Quinazolines / chemistry*
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Streptococcus pyogenes / enzymology
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Quinazolines
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DNA
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DNA Polymerase III