Source:http://linkedlifedata.com/resource/pubmed/id/17201410
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2007-1-4
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pubmed:abstractText |
2-Aminopyridine-3,5-dicarbonitrile compounds were previously identified as mimetics of dominant-negative prion protein mutants and inhibit prion replication in cultured cells. Here, we report findings from a comprehensive structure-activity relationship study of the 6-aminopyridine-3,5-dicarbonitrile scaffold. We identify compounds with significantly improved bioactivity (approximately 40-fold) against replication of the infectious prion isoform (PrPSc) and suitable pharmacokinetic profiles to warrant evaluation in animal models of prion disease.
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pubmed:grant | |
pubmed:commentsCorrections | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
11
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pubmed:volume |
50
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
65-73
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:17201410-Aminopyridines,
pubmed-meshheading:17201410-Animals,
pubmed-meshheading:17201410-Cell Line, Tumor,
pubmed-meshheading:17201410-Combinatorial Chemistry Techniques,
pubmed-meshheading:17201410-Membranes, Artificial,
pubmed-meshheading:17201410-Mice,
pubmed-meshheading:17201410-Models, Molecular,
pubmed-meshheading:17201410-Nitriles,
pubmed-meshheading:17201410-Permeability,
pubmed-meshheading:17201410-PrPSc Proteins,
pubmed-meshheading:17201410-Solubility,
pubmed-meshheading:17201410-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
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pubmed:affiliation |
Institute for Neurodegenerative Diseases, University of California-San Francisco, San Francisco, California 94158, USA. bmay@ind.ucsf.edu
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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