| Title : Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular docking of new acridine-coumarin hybrids - Hamulakova_2017_Int.J.Biol.Macromol_104_333 |
| Author(s) : Hamulakova S , Janovec L , Soukup O , Jun D , Kuca K |
| Ref : Int J Biol Macromol , 104 :333 , 2017 |
|
Abstract :
A novel series of acridine-coumarin hybrids was synthesized and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The newly synthesized derivatives 9a-d have shown higher activity against human AChE (hAChE) compared with 7-MEOTA as the standard drug. Among them derivative 9b exhibited the most potent acetylcholinesterase inhibitory activity, with an IC50 value of 5.85muM compared with 7-MEOTA (IC50=15muM). Molecular modelling studies were performed to predict the binding modes of compounds 9b, 9c and 9f with hAChE/hBuChE. |
| PubMedSearch : Hamulakova_2017_Int.J.Biol.Macromol_104_333 |
| PubMedID: 28601645 |
Hamulakova S, Janovec L, Soukup O, Jun D, Kuca K (2017)
Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular docking of new acridine-coumarin hybrids
Int J Biol Macromol
104 :333
Hamulakova S, Janovec L, Soukup O, Jun D, Kuca K (2017)
Int J Biol Macromol
104 :333