| Title : Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives - Yan_2009_Bioorg.Med.Chem_17_6937 |
| Author(s) : Yan J , Sun L , Wu G , Yi P , Yang F , Zhou L , Zhang X , Li Z , Yang X , Luo H , Qiu M |
| Ref : Bioorganic & Medicinal Chemistry , 17 :6937 , 2009 |
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Abstract :
By targeting multi-active sites of acetylcholinesterase (AChE), a series of huperzine A (Hup A) derivatives with various aromatic ring groups were designed and synthesized by Schiff reaction. They were evaluated as AChE and butyrylcholinesterase (BChE) inhibitors. Results showed very significant specificity that the group of imine derivatives could inhibit TcAChE and hAChE, but no inhibitory effect on hBChE was detected. The experiment was explained by a docking study. In the docking model, we confirmed that aromatic ring of Hup A derivatives played the pi-pi stacking against aminophenol residues of AChE, and the structure-activity relationship (SAR) was discussed. |
| PubMedSearch : Yan_2009_Bioorg.Med.Chem_17_6937 |
| PubMedID: 19726199 |
Yan J, Sun L, Wu G, Yi P, Yang F, Zhou L, Zhang X, Li Z, Yang X, Luo H, Qiu M (2009)
Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives
Bioorganic & Medicinal Chemistry
17 :6937
Yan J, Sun L, Wu G, Yi P, Yang F, Zhou L, Zhang X, Li Z, Yang X, Luo H, Qiu M (2009)
Bioorganic & Medicinal Chemistry
17 :6937