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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2010-7-27
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pubmed:abstractText |
Herein we describe further evolution of hydroxyethylamine inhibitors of BACE-1 with enhanced permeability characteristics necessary for CNS penetration. Variation at the P2' position of the inhibitor with more polar substituents led to compounds 19 and 32, which retained the potency of more lipophilic analog 1 but with much higher observed passive permeability in MDCK cellular assay.
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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 |
Aug
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AquinoJoseJ,
pubmed-author:ArtisDean RDR,
pubmed-author:BovaMichael PMP,
pubmed-author:BrechtEricE,
pubmed-author:BrogleyLouisL,
pubmed-author:DappenMichael SMS,
pubmed-author:FangLarryL,
pubmed-author:HomRoy KRK,
pubmed-author:JohnVargheseV,
pubmed-author:KonradiAndrei WAW,
pubmed-author:NauRR,
pubmed-author:PleissMichael AMA,
pubmed-author:ProbstGary DGD,
pubmed-author:QuinnKevin PKP,
pubmed-author:RuslimLanyL,
pubmed-author:SauerJohn-MichaelJM,
pubmed-author:SealyJennifer MJM,
pubmed-author:ShamHing LHL,
pubmed-author:SinhaSukantoS,
pubmed-author:TóthGergleyG,
pubmed-author:TruongAnh PAP,
pubmed-author:TuckerJohn AJA,
pubmed-author:TungJay SJS,
pubmed-author:YaoNanhuaN,
pubmed-author:YednockTed ATA,
pubmed-author:ZmolekWesW
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pubmed:copyrightInfo |
2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4789-94
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pubmed:meshHeading |
pubmed-meshheading:20634069-Acetamides,
pubmed-meshheading:20634069-Amyloid Precursor Protein Secretases,
pubmed-meshheading:20634069-Aspartic Acid Endopeptidases,
pubmed-meshheading:20634069-Binding Sites,
pubmed-meshheading:20634069-Butanols,
pubmed-meshheading:20634069-Cell Membrane Permeability,
pubmed-meshheading:20634069-Crystallography, X-Ray,
pubmed-meshheading:20634069-Cyclohexylamines,
pubmed-meshheading:20634069-Humans,
pubmed-meshheading:20634069-Protease Inhibitors,
pubmed-meshheading:20634069-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.
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pubmed:affiliation |
Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, CA 94080, United States.
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pubmed:publicationType |
Journal Article
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