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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
2003-3-6
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pubmed:abstractText |
The discovery of a novel class of nitric oxide synthase (NOS) inhibitors, 2-substituted 1,2-dihydro-4-quinazolinamines, and the related 4'-aminospiro[piperidine-4,2'(1'H)-quinazolin]-4'-amines is described. Members of both series exhibit nanomolar potency and high selectivity for the inducible isoform of the enzyme (i-NOS) relative to the constitutive isoforms in vitro. Efficacy in acute and chronic animal models of inflammatory disease following oral administration has also been demonstrated using these compounds.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BeatonHaydn GHG,
pubmed-author:Boughton-SmithNigelN,
pubmed-author:CookTony RTR,
pubmed-author:CooperSally LSL,
pubmed-author:Fraser-RaeLynneL,
pubmed-author:HallamKayK,
pubmed-author:HamleyPeterP,
pubmed-author:McInallyTomT,
pubmed-author:NichollsDavid JDJ,
pubmed-author:PimmAusten DAD,
pubmed-author:TinkerAlan CAC,
pubmed-author:WallaceAlan VAV
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pubmed:issnType |
Print
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pubmed:day |
13
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
913-6
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:12620067-Acute Disease,
pubmed-meshheading:12620067-Administration, Oral,
pubmed-meshheading:12620067-Amines,
pubmed-meshheading:12620067-Animals,
pubmed-meshheading:12620067-Arthritis, Experimental,
pubmed-meshheading:12620067-Cell Line,
pubmed-meshheading:12620067-Chronic Disease,
pubmed-meshheading:12620067-Enzyme Inhibitors,
pubmed-meshheading:12620067-Injections, Intravenous,
pubmed-meshheading:12620067-Isoenzymes,
pubmed-meshheading:12620067-Nitric Oxide Synthase,
pubmed-meshheading:12620067-Nitric Oxide Synthase Type II,
pubmed-meshheading:12620067-Quinazolines,
pubmed-meshheading:12620067-Rats,
pubmed-meshheading:12620067-Spiro Compounds,
pubmed-meshheading:12620067-Structure-Activity Relationship
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pubmed:year |
2003
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pubmed:articleTitle |
1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.
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pubmed:affiliation |
Department of Medicinal Chemistry, AstraZeneca R & D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK. Alan.C.Tinker@Astrazeneca.com
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pubmed:publicationType |
Journal Article
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