title: The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).
abstract: By careful analysis of experimental X-ray ligand crystallographic protein data across several inhibitor series we have discovered a novel, potent and selective series of iNOS inhibitors exemplified by compound 8.
authors.affiliation: Department of Chemistry, AstraZeneca Charnwood, Bakewell Road, Loughborough LE11 5RH, United Kingdom. dave.cheshire@astrazeneca.com
authors.forename: David R
authors.initials: DR
authors.lastname: Cheshire
authors.forename: Anders
authors.initials: A
authors.lastname: Åberg
authors.forename: Gunilla M K
authors.initials: GM
authors.lastname: Andersson
authors.forename: Glen
authors.initials: G
authors.lastname: Andrews
authors.forename: Haydn G
authors.initials: HG
authors.lastname: Beaton
authors.forename: Timothy N
authors.initials: TN
authors.lastname: Birkinshaw
authors.forename: Nigel
authors.initials: N
authors.lastname: Boughton-Smith
authors.forename: Stephen
authors.initials: S
authors.lastname: Connolly
authors.forename: Tony R
authors.initials: TR
authors.lastname: Cook
authors.forename: Anne
authors.initials: A
authors.lastname: Cooper
authors.forename: Sally L
authors.initials: SL
authors.lastname: Cooper
authors.forename: David
authors.initials: D
authors.lastname: Cox
authors.forename: John
authors.initials: J
authors.lastname: Dixon
authors.forename: Nigel
authors.initials: N
authors.lastname: Gensmantel
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Hamley
authors.forename: Richard
authors.initials: R
authors.lastname: Harrison
authors.forename: Paul
authors.initials: P
authors.lastname: Hartopp
authors.forename: Helena
authors.initials: H
authors.lastname: Käck
authors.forename: Paul D
authors.initials: PD
authors.lastname: Leeson
authors.forename: Timothy
authors.initials: T
authors.lastname: Luker
authors.forename: Antonio
authors.initials: A
authors.lastname: Mete
authors.forename: Ian
authors.initials: I
authors.lastname: Millichip
authors.forename: David J
authors.initials: DJ
authors.lastname: Nicholls
authors.forename: Austen D
authors.initials: AD
authors.lastname: Pimm
authors.forename: Steve A
authors.initials: SA
authors.lastname: St-Gallay
authors.forename: Alan V
authors.initials: AV
authors.lastname: Wallace
mesh_terms: D000818:Animals; D001665:Binding Sites; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D008862:Microsomes, Liver / Q000378:metabolism; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017434:Protein Structure, Tertiary; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats
chemical_list: D004791:Enzyme Inhibitors; D007555:Isoxazoles; D011725:Pyridines; D052247:Nitric Oxide Synthase Type II