title: Quinazolin-2-ylamino-quinazolin-4-ols as novel non-nucleoside inhibitors of bacterial DNA polymerase III.
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.
authors.affiliation: Replidyne, Inc., 1450 Infinite Dr., Louisville, CO 80027, USA. joe.guiles@comcast.net
authors.forename: Joseph
authors.initials: J
authors.lastname: Guiles
authors.forename: Xicheng
authors.initials: X
authors.lastname: Sun
authors.forename: Ian A
authors.initials: IA
authors.lastname: Critchley
authors.forename: Urs
authors.initials: U
authors.lastname: Ochsner
authors.forename: Ming
authors.initials: M
authors.lastname: Tregay
authors.forename: Kim
authors.initials: K
authors.lastname: Stone
authors.forename: Jennifer
authors.initials: J
authors.lastname: Bertino
authors.forename: Louis
authors.initials: L
authors.lastname: Green
authors.forename: Rob
authors.initials: R
authors.lastname: Sabin
authors.forename: Frank
authors.initials: F
authors.lastname: Dean
authors.forename: H Garry
authors.initials: HG
authors.lastname: Dallmann
authors.forename: Charles S
authors.initials: CS
authors.lastname: McHenry
authors.forename: Nebojsa
authors.initials: N
authors.lastname: Janjic
mesh_terms: D016923:Cell Death; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004247:DNA / Q000737:chemistry; D004258:DNA Polymerase III / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D008954:Models, Biological; D008956:Models, Chemical; D015394:Molecular Structure; D011799:Quinazolines / Q000737:chemistry*; D013297:Streptococcus pyogenes / Q000201:enzymology; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011799:Quinazolines; D004247:DNA; D004258:DNA Polymerase III