| Title : Design and synthesis of benzodiazepine-1,2,3-triazole hybrid derivatives as selective butyrylcholinesterase inhibitors - Mehrazar_2020_Mol.Divers_24_997 |
| Author(s) : Mehrazar M , Hassankalhori M , Toolabi M , Goli F , Moghimi S , Nadri H , Bukhari SNA , Firoozpour L , Foroumadi A |
| Ref : Mol Divers , 24 :997 , 2020 |
|
Abstract :
A new series of compounds based on benzodiazepine-1,2,3-triazole were synthesized and evaluated as cholinesterase inhibitors by Ellman's method. The compounds proved to be selective inhibitors of butyrylcholinesterase (BuChE) over acetylcholinesterase. The most potent compound was 3,3-dimethyl-11-(3-((1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-2,3,4,5,10,11-hexahydro-1H-dibenzo[b,e][1,4]diazepin-1-one, identified as a submicromolar inhibitor of BuChE with IC(50) value of 0.2 microM. In addition, the amyloid-beta self-aggregation evaluation studies for selected compounds showed potent inhibitory effects compared to donepezil. The docking and cell viability studies supported the potential of compound 9b-6 as significant BuChE inhibitor. |
| PubMedSearch : Mehrazar_2020_Mol.Divers_24_997 |
| PubMedID: 31845210 |
Mehrazar M, Hassankalhori M, Toolabi M, Goli F, Moghimi S, Nadri H, Bukhari SNA, Firoozpour L, Foroumadi A (2020)
Design and synthesis of benzodiazepine-1,2,3-triazole hybrid derivatives as selective butyrylcholinesterase inhibitors
Mol Divers
24 :997
Mehrazar M, Hassankalhori M, Toolabi M, Goli F, Moghimi S, Nadri H, Bukhari SNA, Firoozpour L, Foroumadi A (2020)
Mol Divers
24 :997