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Bioorg Med Chem Lett ; 19(3): 800-2, 2009 Feb 01.
Article in English | MEDLINE | ID: mdl-19109016

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.


Subject(s)
Chemistry, Pharmaceutical/methods , DNA Polymerase III/antagonists & inhibitors , DNA Polymerase III/chemistry , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Quinazolines/chemistry , Cell Death , DNA/chemistry , Drug Design , Drug Evaluation, Preclinical , Humans , Models, Biological , Models, Chemical , Molecular Structure , Streptococcus pyogenes/enzymology , Structure-Activity Relationship
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