Synthesis of Novel 4-(Dimethylaminoalkyl)piperazine-1-carbodithioa t e Derivatives as Cholinesterase Inhibitors

Title:Synthesis of Novel 4-(Dimethylaminoalkyl)piperazine-1-carbodithioa t e Derivatives as Cholinesterase Inhibitors

Volume: 14 Issue: 5

Author(s): Ulviye Acar Cevik, Serkan Levent, Begum Nurpelin Saglık, Yusuf Ozkay*Zafer Asım Kaplancıklı

Affiliation:

• Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Yunus Emre Campus, 26470 Tepebaşı/Eskisehir,Turkey

Keywords: Piperazine, dithiocarbamate, acetylcholinesterase, butyrylcholinesterase, enzyme.

Abstract: Background: Carbamate compounds have attracted a great deal of interest in medicinal chemistry due to their inhibition potential against cholinesterase enzymes.

Method: Hence, this study was undertaken to synthesize new piperazine derivatives including dithiocarbamate moiety, which is the bioisoster of carbamate. Twenty eight 4-(dimethylaminoalkyl) piperazine-1-carbodithioate derivatives (3a-3n, 4a-4n) were synthesized. Chemical structures of these compounds were confirmed by spectral data. Ellman’s assay was applied in order to investigate inhibitory potency of the compounds against Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE) enzymes.

Results and Conclusion: It was determined that some of the compounds have remarkable activity on AChE. ADME (Absorption, distribution, metabolism, elimination) predictions were theoretically performed for all compounds in the series. Enzyme kinetics and molecular docking studies were carried out for the most active compound (3n) and nature of inhibition and interactions between enzyme and ligand were described.

Cite this article as:

Cevik Acar Ulviye, Levent Serkan, Saglık Nurpelin Begum, Ozkay Yusuf*, Kaplancıklı Asım Zafer, Synthesis of Novel 4-(Dimethylaminoalkyl)piperazine-1-carbodithioa t e Derivatives as Cholinesterase Inhibitors, Letters in Drug Design & Discovery 2017; 14 (5) . https://dx.doi.org/10.2174/1570180813666160923105636

DOI https://dx.doi.org/10.2174/1570180813666160923105636	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X