Document Detail


NSAID-derived γ-secretase modulation requires an acidic moiety on the carbazole scaffold.
MedLine Citation:
PMID:  21763147     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Modulation of γ-secretase activity holds potential for the treatment of Alzheimer's disease. Most NSAID-derived γ-secretase modulators feature a carboxylic acid, which may impair blood-brain barrier permeation. The structure activity relationship of 33 carbazoles featuring diverse carboxylic acid isosteres or metabolic precursors thereof was established in a cellular amyloid secretion assay. The modulatory activity was observed for acidic moieties and metabolically labile esters only, which supports our hypothesis of an acid-lysine interaction to be relevant for this type of γ-secretase modulators.
Authors:
Andrea Zall; Daniel Kieser; Nicole Höttecke; Eva C Naumann; Binia Thomaszewski; Katrin Schneider; Dirk T Steinbacher; Robert Schubenel; Stefan Masur; Karlheinz Baumann; Boris Schmidt
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-6-29
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  -     ISSN:  1464-3391     ISO Abbreviation:  -     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-7-18     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
Clemens Schöpf-Institute of Chemistry and Biochemistry, Technische Universität Darmstadt, Petersenstr. 22, Darmstadt D-64287, Germany.
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