| Title : Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease - Rahim_2015_Bioorg.Chem_62_106 |
| Author(s) : Rahim F , Javed MT , Ullah H , Wadood A , Taha M , Ashraf M , Qurat Ul A , Khan MA , Khan F , Mirza S , Khan KM |
| Ref : Bioorg Chem , 62 :106 , 2015 |
|
Abstract :
A series of thirty (30) thiazole analogs were prepared, characterized by 1H NMR, 13C NMR and EI-MS and evaluated for Acetylcholinesterase and butyrylcholinesterase inhibitory potential. All analogs exhibited varied butyrylcholinesterase inhibitory activity with IC50 value ranging between 1.59+/-0.01 and 389.25+/-1.75muM when compared with the standard eserine (IC50, 0.85+/-0.0001muM). Analogs 15, 7, 12, 9, 14, 1, 30 with IC50 values 1.59+/-0.01, 1.77+/-0.01, 6.21+/-0.01, 7.56+/-0.01, 8.46+/-0.01, 14.81+/-0.32 and 16.54+/-0.21muM respectively showed excellent inhibitory potential. Seven analogs 15, 20, 19, 24, 28, 30 and 25 exhibited good acetylcholinesterase inhibitory potential with IC50 values 21.3+/-0.50, 35.3+/-0.64, 36.6+/-0.70, 44.81+/-0.81, 46.36+/-0.84, 48.2+/-0.06 and 48.72+/-0.91muM respectively. All other analogs also exhibited well to moderate enzyme inhibition. The binding mode of these compounds was confirmed through molecular docking. |
| PubMedSearch : Rahim_2015_Bioorg.Chem_62_106 |
| PubMedID: 26318401 |
Rahim F, Javed MT, Ullah H, Wadood A, Taha M, Ashraf M, Qurat Ul A, Khan MA, Khan F, Mirza S, Khan KM (2015)
Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
Bioorg Chem
62 :106
Rahim F, Javed MT, Ullah H, Wadood A, Taha M, Ashraf M, Qurat Ul A, Khan MA, Khan F, Mirza S, Khan KM (2015)
Bioorg Chem
62 :106