Rational approach to discover multipotent anti-Alzheimer drugs

被引:232
作者
Rosini, M
Andrisano, V
Bartolini, M
Bolognesi, ML
Hrelia, P
Minarini, A
Tarozzi, A
Melchiorre, C
机构
[1] Univ Bologna, Dept Pharmaceut Sci, I-40126 Bologna, Italy
[2] Univ Bologna, Dept Pharmacol, I-40126 Bologna, Italy
关键词
D O I
10.1021/jm049112h
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The coupling of two different pharmacophores, each endowed with different biological properties, afforded the hybrid compound lipocrine (7), whose biological profile was markedly improved relative to those of prototypes tacrine and lipoic acid. Lipocrine is the first compound that inhibits the catalytic activity of AChE and AChE-induced amyloid-beta aggregation and protects against reactive oxygen species. Thus, it emerged as a valuable pharmacological tool to investigate Alzheimer's disease and as a promising lead compound for new anti-Alzheimer drugs.
引用
收藏
页码:360 / 363
页数:4
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