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

Mohsen U., KAPLANCIKLI Z. A., ÖZKAY Y., Yurttä L.

Drug Research, cilt.65, sa.4, ss.176-183, 2015 (ESCI) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 65 Sayı: 4
  • Basım Tarihi: 2015
  • Doi Numarası: 10.1055/s-0034-1375613
  • Dergi Adı: Drug Research
  • Derginin Tarandığı İndeksler: Emerging Sources Citation Index (ESCI), Scopus
  • Sayfa Sayıları: ss.176-183
  • Anahtar Kelimeler: benzothiazole, piperazine, dithiocarbamate, cholinesterase inhibitors, ALZHEIMERS-DISEASE, CHOLINESTERASE-INHIBITORS, ACETYLCHOLINESTERASE INHIBITORS, DESIGN, AGENTS, ANTIBACTERIAL, EFFICACY, HYBRIDS
  • Anadolu Üniversitesi Adresli: Evet

Özet

© Georg Thieme Verlag KG Stuttgart.Abstract 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, 1H-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.