NSAID-derived γ-secretase modulation requires an acidic moiety on the carbazole scaffold
摘要：
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.
展开
DOI：
10.1016/j.bmc.2011.06.062
被引量：
年份：
2011
相似文献
参考文献
引证文献
来源期刊
引用走势
2013
被引量：18
站内活动
辅助模式
0
引用
文献可以批量引用啦~
欢迎点我试用！
