- The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent.
The geminal dimethyl analogue of Flurbiprofen as a novel Abeta42 inhibitor and potential Alzheimer's disease modifying agent.
Bioorganic & medicinal chemistry letters (2006-02-04)
Nicholas Stock, Benito Munoz, Jonathan D J Wrigley, Mark S Shearman, Dirk Beher, James Peachey, Toni L Williamson, Gretchen Bain, Weichao Chen, Xiaohui Jiang, René St-Jacques, Peppi Prasit
PMID16455248
摘要
The subtle modification of a selection of Abeta42 inhibiting non-steroidal anti-inflammatory drugs (NSAIDs), through synthesis of the geminal dimethyl analogues, was anticipated to ablate their cyclooxygenase activity whilst maintaining Abeta42 inhibition. Methylflurbiprofen 6 exhibited similar in vitro Abeta42 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.
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