| Title : A Novel Class of Selective Acetylcholinesterase Inhibitors: Synthesis and Evaluation of (E)-2-(Benzo[d]thiazol-2-yl)-3-heteroarylacrylonitriles - Torre_2012_Molecules_17_12072 |
| Author(s) : Torre Pde L , Saavedra LA , Caballero J , Quiroga J , Alzate-Morales JH , Cabrera MG , Trilleras J |
| Ref : Molecules , 17 :12072 , 2012 |
|
Abstract :
(E)-2-(benzo[d]thiazol-2-yl)-3-heteroarylacrylonitriles are described as a new class of selective inhibitors of acetylcholinesterase AChE The most potent compound in the series exhibited good AChE inhibitory activity IC(50 64 micro;M Compound 7f was found to be more selective than galanthamine in inhibiting AChE and it showed a moderate selectivity index Kinetic studies on AChE indicated that a competitive type of inhibition pattern exist for these acrylonitrile derivates Molecular docking models of the ligand-AChE complexes suggest that compound 7g is located on the periphery of the AChE active site. |
| PubMedSearch : Torre_2012_Molecules_17_12072 |
| PubMedID: 23085657 |
Torre Pde L, Saavedra LA, Caballero J, Quiroga J, Alzate-Morales JH, Cabrera MG, Trilleras J (2012)
A Novel Class of Selective Acetylcholinesterase Inhibitors: Synthesis and Evaluation of (E)-2-(Benzo[d]thiazol-2-yl)-3-heteroarylacrylonitriles
Molecules
17 :12072
Torre Pde L, Saavedra LA, Caballero J, Quiroga J, Alzate-Morales JH, Cabrera MG, Trilleras J (2012)
Molecules
17 :12072