rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
11
|
pubmed:dateCreated |
1999-3-11
|
pubmed:abstractText |
Matrix metalloproteinase inhibitors of general formula (1) were synthesised by a route involving an Ireland-Claisen rearrangement which enables systematic modification of the substituent alpha to the hydroxamic acid. An analogue (12c) possessing an alpha-cyclopentyl group is a potent broad spectrum inhibitor that displays high and sustained blood levels following oral dosing in both the rat and marmoset ex-vivo bioassays. This compound and analogues are also potent inhibitors of TNF alpha release.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
0960-894X
|
pubmed:author |
pubmed-author:BeckettR PRP,
pubmed-author:BellamyC LCL,
pubmed-author:CorkillD JDJ,
pubmed-author:CossinsJJ,
pubmed-author:CourtneyP FPF,
pubmed-author:DavidsonA HAH,
pubmed-author:DaviesS JSJ,
pubmed-author:DrummondA HAH,
pubmed-author:HelfrichKK,
pubmed-author:LewisC NCN,
pubmed-author:ManganMM,
pubmed-author:MartinF MFM,
pubmed-author:MillerKK,
pubmed-author:NayeePP,
pubmed-author:PrattL MLM,
pubmed-author:RickettsM LML,
pubmed-author:ThomasWW,
pubmed-author:ToddR SRS,
pubmed-author:WhittakerMM
|
pubmed:issnType |
Print
|
pubmed:day |
2
|
pubmed:volume |
8
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1359-64
|
pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9871766-Administration, Oral,
pubmed-meshheading:9871766-Animals,
pubmed-meshheading:9871766-Biological Availability,
pubmed-meshheading:9871766-Callithrix,
pubmed-meshheading:9871766-Depression, Chemical,
pubmed-meshheading:9871766-Hydroxamic Acids,
pubmed-meshheading:9871766-Lipopolysaccharides,
pubmed-meshheading:9871766-Metalloendopeptidases,
pubmed-meshheading:9871766-Protease Inhibitors,
pubmed-meshheading:9871766-Rats,
pubmed-meshheading:9871766-Tumor Necrosis Factor-alpha
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pubmed:year |
1998
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pubmed:articleTitle |
The synthesis of novel matrix metalloproteinase inhibitors employing the Ireland-Claisen rearrangement.
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pubmed:affiliation |
British Biotech Pharmaceuticals Limited, Cowley, Oxford.
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pubmed:publicationType |
Journal Article
|