| Title : O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-beta aggregation - Mao_2012_Bioorg.Med.Chem_20_5884 |
| Author(s) : Mao F , Huang L , Luo Z , Liu A , Lu C , Xie Z , Li X |
| Ref : Bioorganic & Medicinal Chemistry , 20 :5884 , 2012 |
| Abstract : In an effort to identify novel multifunctional drug candidates for the treatment of Alzheimer's disease (AD), a series of hybrid molecules were synthesised by reacting N-(aminoalkyl)tacrine with salicylic aldehyde or derivatives of 2-aminobenzaldehyde. These compounds were then evaluated as multifunctional anti-Alzheimer's disease agents. All of the hybrids are potential biometal chelators, and in addition, most of them were better antioxidants and inhibitors of cholinesterases and amyloid-beta (Abeta) aggregation than the lead compound tacrine. Compound 7c has the potential to be a candidate for AD therapy: it is a much better inhibitor of acetylcholinesterase (AChE) than tacrine (IC(50): 0.55 nM vs 109 nM), has good biometal chelation ability, is able to inhibit Abeta aggregation and has moderate antioxidant activity (1.22 Trolox equivalents). |
| ESTHER : Mao_2012_Bioorg.Med.Chem_20_5884 |
| PubMedSearch : Mao_2012_Bioorg.Med.Chem_20_5884 |
| PubMedID: 22944335 |
Mao F, Huang L, Luo Z, Liu A, Lu C, Xie Z, Li X (2012)
O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-beta aggregation
Bioorganic & Medicinal Chemistry
20 :5884
Mao F, Huang L, Luo Z, Liu A, Lu C, Xie Z, Li X (2012)
Bioorganic & Medicinal Chemistry
20 :5884