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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
2009-10-26
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pubmed:abstractText |
Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar Abeta cellular inhibition with selectivity against cathepsin-D. X-ray crystallography illuminated the S1' residues critical to this effort, which culminated in compounds 56 and 57 that exhibited potency and selectivity but poor permeability and high P-gp efflux.
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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 |
Nov
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AquinoJoseJ,
pubmed-author:BovaMichael PMP,
pubmed-author:BrogleyLouisL,
pubmed-author:DappenMichael SMS,
pubmed-author:DressenDarrenD,
pubmed-author:HomRoy KRK,
pubmed-author:JagodzinskaBarbara MBM,
pubmed-author:JimMillerM,
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:SinhaSukantoS,
pubmed-author:TothGergelyG,
pubmed-author:TruongAnh PAP,
pubmed-author:TsoLukeL,
pubmed-author:TuckerJohn AJA,
pubmed-author:TungJay SJS,
pubmed-author:WoneDavid W GDW
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6386-91
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pubmed:meshHeading |
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pubmed:year |
2009
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pubmed:articleTitle |
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.
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pubmed:affiliation |
Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, CA 94080, USA.
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pubmed:publicationType |
Journal Article
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