Basiri_2014_Bioorg.Med.Chem_22_906

Reference

Title : Cholinesterase inhibitory activity versus aromatic core multiplicity: A facile green synthesis and molecular docking study of novel piperidone embedded thiazolopyrimidines - Basiri_2014_Bioorg.Med.Chem_22_906
Author(s) : Basiri A , Murugaiyah V , Osman H , Kumar RS , Kia Y , Hooda A , Parsons RB
Ref : Bioorganic & Medicinal Chemistry , 22 :906 , 2014
Abstract :

Novel thiazolopyrimidine derivatives have been synthesized via microwave assisted, domino cascade methodology in ionic liquid and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Among the newly synthesized compounds 6d, 6a, 6e and 6b displayed higher AChE inhibitory activity than standard drug, galanthamine, with IC50 values of 0.53, 1.47, 1.62 and 2.05muM, respectively. Interestingly, all the compounds except for 6m-r and 6x displayed higher BChE inhibitory potentials than galanthamine with IC50 values ranging from 1.09 to 18.56muM. Molecular docking simulations for 6d possessing the most potent AChE and BChE inhibitory activities, disclosed its binding interactions at the active site gorge of AChE and BChE enzymes.

PubMedSearch : Basiri_2014_Bioorg.Med.Chem_22_906
PubMedID: 24369842

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Citations formats

Basiri A, Murugaiyah V, Osman H, Kumar RS, Kia Y, Hooda A, Parsons RB (2014)
Cholinesterase inhibitory activity versus aromatic core multiplicity: A facile green synthesis and molecular docking study of novel piperidone embedded thiazolopyrimidines
Bioorganic & Medicinal Chemistry 22 :906

Basiri A, Murugaiyah V, Osman H, Kumar RS, Kia Y, Hooda A, Parsons RB (2014)
Bioorganic & Medicinal Chemistry 22 :906