| Title : AChE inhibitor: a regio- and stereo-selective 1,3-dipolar cycloaddition for the synthesis of novel substituted 5,6-dimethoxy spiro[5.3']-oxindole-spiro-[6.3'']-2,3-dihydro-1H-inden-1''-one-7-(substituted aryl)-tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole - Ashraf_2012_Bioorg.Med.Chem.Lett_22_508 |
| Author(s) : Ashraf Ali M , Ismail R , Choon TS , Kumar RS , Osman H , Arumugam N , Almansour AI , Elumalai K , Singh A |
| Ref : Bioorganic & Medicinal Chemistry Lett , 22 :508 , 2012 |
|
Abstract :
Pyrrolothiazolyloxindole analogues share vital pharmacological properties, considered useful in Alzheimer's disease (AD). The aim of this study was synthesis and evaluate pyralothiazolyloxindole analogues if possess acetyl cholinesterase (AChE) inhibitory activity. The easily accessible one-pot synthesis of these compounds resulted to be significantly less difficult and expensive than that of donepezil. Several compounds possess anti-cholinesterase activity in the order of micro and sub-micromolar. Particularly, compound was the most potent inhibitors of the series against acetyl cholinesterase enzyme with IC(50) 0.11mumol/L. |
| PubMedSearch : Ashraf_2012_Bioorg.Med.Chem.Lett_22_508 |
| PubMedID: 22142546 |
Ashraf Ali M, Ismail R, Choon TS, Kumar RS, Osman H, Arumugam N, Almansour AI, Elumalai K, Singh A (2012)
AChE inhibitor: a regio- and stereo-selective 1,3-dipolar cycloaddition for the synthesis of novel substituted 5,6-dimethoxy spiro[5.3']-oxindole-spiro-[6.3'']-2,3-dihydro-1H-inden-1''-one-7-(substituted aryl)-tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole
Bioorganic & Medicinal Chemistry Lett
22 :508
Ashraf Ali M, Ismail R, Choon TS, Kumar RS, Osman H, Arumugam N, Almansour AI, Elumalai K, Singh A (2012)
Bioorganic & Medicinal Chemistry Lett
22 :508