کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10582682 | 981085 | 2011 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
NSAID-derived γ-secretase modulation requires an acidic moiety on the carbazole scaffold
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 16, 15 August 2011, Pages 4903-4909
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 16, 15 August 2011, Pages 4903-4909
نویسندگان
Andrea Zall, Daniel Kieser, Nicole Höttecke, Eva C. Naumann, Binia Thomaszewski, Katrin Schneider, Dirk T. Steinbacher, Robert Schubenel, Stefan Masur, Karlheinz Baumann, Boris Schmidt,