| Title : Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors - Tang_2007_Bioorg.Med.Chem.Lett_17_3765 |
| Author(s) : Tang H , Ning FX , Wei YB , Huang SL , Huang ZS , Chan AS , Gu LQ |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :3765 , 2007 |
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Abstract :
A series of 9-aminoalkanamido-1-azabenzanthrones derviatives (3a-i Ar-NHCO(CH(2))(n)NR(1)R(2)) and their quaternary methiodide salts (4a-g Ar-NHCO(CH(2))(n)N(+)(CH(3))R(1)R(2)I(-)) were designed and synthesized as acetylcholinesterase (AChE) or butyrylcholinesterase (BuChE) inhibitors. The synthetic compounds exhibited high AChE inhibitory activity with IC(50) values in the nanomolar range and high selectivity for AChE over BuChE (45- to 1980-fold). The structure-activity relationships (SARs) were discussed. |
| PubMedSearch : Tang_2007_Bioorg.Med.Chem.Lett_17_3765 |
| PubMedID: 17451950 |
Tang H, Ning FX, Wei YB, Huang SL, Huang ZS, Chan AS, Gu LQ (2007)
Derivatives of oxoisoaporphine alkaloids: a novel class of selective acetylcholinesterase inhibitors
Bioorganic & Medicinal Chemistry Lett
17 :3765
Tang H, Ning FX, Wei YB, Huang SL, Huang ZS, Chan AS, Gu LQ (2007)
Bioorganic & Medicinal Chemistry Lett
17 :3765