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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2003-9-5
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pubmed:abstractText |
Several beta-secretase inhibitors were designed based on hydroxyethylamine dipeptide isostere (HDI) structures and were synthesized by a methodology using the aza-Payne rearragement and O,N-acyl transfer reactions to study their structure-activity relationships. Among these pseudopeptides, effective compounds were developed as the first beta-secretase inhibitors containing the HDI transition state mimic with potent enzyme inhibitory activity (IC50 < 100 nM).
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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 |
Jul
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pubmed:issn |
1477-0520
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
1
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2468-73
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:12956063-Acylation,
pubmed-meshheading:12956063-Amino Acid Sequence,
pubmed-meshheading:12956063-Aspartic Acid Endopeptidases,
pubmed-meshheading:12956063-Aza Compounds,
pubmed-meshheading:12956063-Dipeptides,
pubmed-meshheading:12956063-Esterification,
pubmed-meshheading:12956063-Ethylamines,
pubmed-meshheading:12956063-Humans,
pubmed-meshheading:12956063-Inhibitory Concentration 50,
pubmed-meshheading:12956063-Isoenzymes,
pubmed-meshheading:12956063-Molecular Mimicry,
pubmed-meshheading:12956063-Oligopeptides,
pubmed-meshheading:12956063-Protease Inhibitors,
pubmed-meshheading:12956063-Recombinant Proteins,
pubmed-meshheading:12956063-Structure-Activity Relationship
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pubmed:year |
2003
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pubmed:articleTitle |
Synthesis of potent beta-secretase inhibitors containing a hydroxyethylamine dipeptide isostere and their structure-activity relationship studies.
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pubmed:affiliation |
Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan. tamamura@pharm.kyoto-u.ac.jp
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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