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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2002-3-7
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pubmed:abstractText |
A study of the S1 binding of lead 5-methylthiothiophene amidine 3, an inhibitor of urokinase-type plasminogen activator, was undertaken by the introduction of a variety of substituents at the thiophene 5-position. The 5-alkyl substituted and unsubstituted thiophenes were prepared using organolithium chemistry. Heteroatom substituents were introduced at the 5-position using a novel displacement reaction of 5-methylsulfonylthiophenes and the corresponding oxygen or sulfur anions. Small alkyl group substitution at the 5-position provided inhibitors equipotent with but possessing improved solubility.
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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 |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BoneRogerR,
pubmed-author:DeckmanIngrid CIC,
pubmed-author:DesJarlaisRenée LRL,
pubmed-author:GrasbergerBruce LBL,
pubmed-author:GreenDavidD,
pubmed-author:HoffmanJames BJB,
pubmed-author:IlligCarl RCR,
pubmed-author:LewandowskiFrankF,
pubmed-author:MaguireDianeD,
pubmed-author:MantheyCarlC,
pubmed-author:MolloyChris JCJ,
pubmed-author:NgoR LRL,
pubmed-author:RandleTroyT,
pubmed-author:RudolphM JonathanMJ,
pubmed-author:SharpCeliaC,
pubmed-author:SollRichard MRM,
pubmed-author:SpurlinoJohn CJC,
pubmed-author:SubasingheNalin LNL,
pubmed-author:WilsonKenneth JKJ,
pubmed-author:ZhangMarieM
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pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
491-5
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
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pubmed:year |
2002
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pubmed:articleTitle |
Design and synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors.
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pubmed:affiliation |
3-Dimensional Pharmaceuticals Inc., 665 Stockton Drive, Exton, PA 19341, USA. rudolph@3dp.com
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pubmed:publicationType |
Journal Article
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