Title : Highly functionalized 2-amino-4H-pyrans as potent cholinesterase inhibitors - Kumar_2018_Bioorg.Chem_81_134 |
Author(s) : Kumar RS , Almansour AI , Arumugam N , Al-Thamili DM , Basiri A , Kotresha D , Manohar TS , Venketesh S , Asad M , Asiri AM |
Ref : Bioorg Chem , 81 :134 , 2018 |
Abstract :
Novel highly functionalized 2-amino-4H-pyrans were achieved in excellent yields under simple grinding at ambient temperature and were assessed for their potential for treating Alzheimer's disease (AD). The 2-amino-4H-pyran bearing nitro groups on both the aryl rings showed the highest activity, with an IC50 of 1.98+/-0.09microM against acetylcholinesterase (AChE) and 10.62+/-0.21microM against butyrylcholinesterase (BChE), the inhibition mechanisms on AChE and BChE receptors were revealed by means of molecular docking simulations. |
PubMedSearch : Kumar_2018_Bioorg.Chem_81_134 |
PubMedID: 30121001 |
Kumar RS, Almansour AI, Arumugam N, Al-Thamili DM, Basiri A, Kotresha D, Manohar TS, Venketesh S, Asad M, Asiri AM (2018)
Highly functionalized 2-amino-4H-pyrans as potent cholinesterase inhibitors
Bioorg Chem
81 :134
Kumar RS, Almansour AI, Arumugam N, Al-Thamili DM, Basiri A, Kotresha D, Manohar TS, Venketesh S, Asad M, Asiri AM (2018)
Bioorg Chem
81 :134