| Title : Design, synthesis and evaluation of novel ferulic acid-memoquin hybrids as potential multifunctional agents for the treatment of Alzheimer's disease - Pan_2016_Bioorg.Med.Chem.Lett_26_2539 |
| Author(s) : Pan W , Hu K , Bai P , Yu L , Ma Q , Li T , Zhang X , Chen C , Peng K , Liu W , Sang Z |
| Ref : Bioorganic & Medicinal Chemistry Lett , 26 :2539 , 2016 |
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Abstract :
A novel series of ferulic acid-memoquin hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease (AD). The in vitro studies showed that most of the compounds exhibited a significant ability to inhibit acetylcholinesterase (AChE) (IC50 of 3.2-34.7muM) and self-induced beta-amyloid (Abeta1-42) aggregation (30.8-39.1%, 25muM), to act as potential antioxidants (ORAC-FL value of 0.9-1.3). In particular, compound 17d had the greatest ability to inhibit AChE (IC50=3.2muM), and Abeta1-42 aggregation (30.8%) was also an excellent antioxidant and neuroprotectant. Moreover, it is capable of disaggregating self-induced Abeta aggregation. Furthermore, 17d could cross the blood-brain barrier (BBB) in vitro. The results showed that compound 17d is a potential multifunctional agent for the treatment of AD. |
| PubMedSearch : Pan_2016_Bioorg.Med.Chem.Lett_26_2539 |
| PubMedID: 27072909 |
| Inhibitor | Memoquin |
Pan W, Hu K, Bai P, Yu L, Ma Q, Li T, Zhang X, Chen C, Peng K, Liu W, Sang Z (2016)
Design, synthesis and evaluation of novel ferulic acid-memoquin hybrids as potential multifunctional agents for the treatment of Alzheimer's disease
Bioorganic & Medicinal Chemistry Lett
26 :2539
Pan W, Hu K, Bai P, Yu L, Ma Q, Li T, Zhang X, Chen C, Peng K, Liu W, Sang Z (2016)
Bioorganic & Medicinal Chemistry Lett
26 :2539