Synthesis and evaluation of anti-acetylcholinesterase activity of some benzothiazole based new piperazine-dithiocarbamate derivatives

• Published in: Drug research Vol. 65; no. 4; p. 176
• Main Authors: Mohsen, U A, Kaplancikli, Z A, Özkay, Y, Yurttaş, L
• Format: Journal Article
• Language: English
• Published: Germany 01.04.2015
• Subjects: Benzothiazoles - chemical synthesis; Benzothiazoles - chemistry; Benzothiazoles - pharmacology; Cholinesterase Inhibitors - chemical synthesis; Cholinesterase Inhibitors - chemistry; Cholinesterase Inhibitors - pharmacology; Indans - pharmacology; Piperazines - chemical synthesis; Piperazines - chemistry; Piperazines - pharmacology; Piperidines - pharmacology; Structure-Activity Relationship; Thiocarbamates - chemical synthesis; Thiocarbamates - chemistry; Thiocarbamates - pharmacology
• ISSN: 2194-9387
• DOI: 10.1055/s-0034-1375613

In this present study some benzothiazole derivatives bearing piperazine and thiocarbamate moieties were synthesized and their potential anticholinesterase properties were investigated. A set of 30 new compounds of 2-[(6-substituted benzothiazol-2-yl)amino]-2-oxoethyl 4-substituted piperazine-1-carbodithioate derivatives were synthesized by reacting 2-chloro-N-(6-substituted benzothiazole-2-yl)acetamide derivatives derivatives and sodium salts of appropriate N,N-disubstituted dithiocarbamic acids in acetone. The structures of the obtained compounds were elucidated using FT-IR, (1)H-NMR and MS spectral data and elemental analyses result. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) using a modificated Ellman's spectrophotometric method. Some of the compounds can be identified as anticholinesterase agents due to their inhibitory effect when compared with Donepezil. Compounds with dimethylamino ethyl or dimethylamino propyl substituents were defined as the anticholinesterase active compounds.