Synthesis of Some New 1(2H)-Phthalazinone Derivatives and Evaluation of Their Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities

Title:Synthesis of Some New 1(2H)-Phthalazinone Derivatives and Evaluation of Their Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities

Volume: 14 Issue: 2

Author(s): Burcu Kılıç, Hayrettin Ozan Gülcan, Mertcan Yalçın, Fatma Aksakal, Anatoli Dimoglo, Mustafa Fethi Şahin and Deniz Songül Doğruer

Affiliation:

Keywords: Alzheimer’s disease, 1(2H)-phthalazinone, acetylcholinesterase inhibitory activity, butyrylcholinesterase inhibitory activity, Ellman’s method, molecular docking.

Abstract: Some 1(2H)-phthalazinone derivatives were synthesized and their chemical structures were confirmed by ¹H-NMR, ¹³C-NMR, mass and elemental analysis. Subsequently, modified Ellman’s method was used to determine both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities of the synthesized compounds. The activity results showed that compound 8c was the most active AChE inhibitor with inhibition value of 63% at 100 μM among the tested compounds. In addition, docking of the synthesized compounds into the active sites of AChE and BuChE was carried out in order to predict the binding energies and non-covalent interactions stabilizing the enzyme-ligand complexes.

Cite this article as:

Kılıç Burcu, Gülcan Ozan Hayrettin, Yalçın Mertcan, Aksakal Fatma, Dimoglo Anatoli, Şahin Fethi Mustafa and Doğruer Songül Deniz, Synthesis of Some New 1(2H)-Phthalazinone Derivatives and Evaluation of Their Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities, Letters in Drug Design & Discovery 2017; 14 (2) . https://dx.doi.org/10.2174/1570180813666160819124611