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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
26
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pubmed:dateCreated |
1997-1-24
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pubmed:abstractText |
The preceding papers of this series detail the development of functionalized indole-3-acetamides as inhibitors of hnps-PLA2. We describe here the extension of the structure-activity relationship to include a series of indole-3-glyoxamide derivatives. Functionalized indole-3-glyoxamides with an acidic substituent appended to the 4- or 5-position of the indole ring were prepared and tested as inhibitors of hnps-PLA2. It was found that the indole-3-glyoxamides with a 4-oxyacetic acid substituent had optimal inhibitory activity. These inhibitors exhibited an improvement in potency over the best of the indole-3-acetamides, and LY315920 (6m) was selected for evaluation clinically as an hnps-PLA2 inhibitor.
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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 |
Dec
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AsayJ LJL,
pubmed-author:CENEKRR,
pubmed-author:CarlsonD GDG,
pubmed-author:ChirgadzeN YNY,
pubmed-author:ClawsonD KDK,
pubmed-author:DillardR DRD,
pubmed-author:DraheimS ESE,
pubmed-author:HartleyL WLW,
pubmed-author:JohnsonL MLM,
pubmed-author:JonesN DND,
pubmed-author:McKinneyE RER,
pubmed-author:MihelichE DED,
pubmed-author:OlkowskiJ LJL,
pubmed-author:SchevitzR WRW,
pubmed-author:SmithA CAC,
pubmed-author:SnyderD WDW,
pubmed-author:SommersC DCD,
pubmed-author:WeryJ PJP
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pubmed:issnType |
Print
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pubmed:day |
20
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pubmed:volume |
39
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5159-75
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
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pubmed:year |
1996
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pubmed:articleTitle |
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.
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pubmed:affiliation |
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
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pubmed:publicationType |
Journal Article
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