Title of article
The geminal dimethyl analogue of Flurbiprofen as a novel Aβ42 inhibitor and potential Alzheimer’s disease modifying agent
Author/Authors
Nicholas Stock، نويسنده , , Benito Munoz، نويسنده , , Jonathan D.J. Wrigley، نويسنده , , Mark S. Shearman، نويسنده , , Dirk Beher، نويسنده , , James Peachey، نويسنده , , Toni L. Williamson، نويسنده , , Gretchen Bain، نويسنده , , Weichao Chen، نويسنده , , Xiaohui Jiang، نويسنده , , René St-Jacques، نويسنده , , Peppi Prasit، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
2219
To page
2223
Abstract
The subtle modification of a selection of Aβ42 inhibiting non-steroidal anti-inflammatory drugs (NSAIDs), through synthesis of the geminal dimethyl analogues, was anticipated to ablate their cyclooxygenase activity whilst maintaining Aβ42 inhibition. Methylflurbiprofen 6 exhibited similar in vitro Aβ42 inhibition to its parent NSAID Flurbiprofen and was further evaluated in the Tg2576 mouse model of Alzheimer’s disease and an animal model of gastro-intestinal (GI) impairment, but proved unviable for further clinical development.
Keywords
Alzheimer’s disease , cyclooxygenase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796753
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