Ditiyiokarbamat Yapısı İçeren Yeni Bazı Benzimidazol Türevlerinin Sentezi ve Potansiyel Kolinesteraz İnhibitörleri olarak Biyolojik Etki Çalışmaları

Amaç: Bu çalışmada, ditiyokarbamat yapısı içeren benzimidazol türevlerinden sekiz yeni madde sentezlenmiş olup, in vitro koşullarda antikolinesteraz aktivitelerinin değerlendirilmesi amaçlanmıştır. Materyal ve Metod: 2-Bromoasetilbenzimidazol ve ditiyokarbamat türevlerinin reaksiyonu sonucu sentezlenen bileşiklerin yapıları 1H-NMR, kütle spektral verileri ayrıca elemental analiz ile aydınlatılmıştır. Ayrıca yapıları tayin edilmiş bileşiklerin Elmann"s spektrofotometrik yöntemiyle asetilkolin esteraz etkileri değerlendirilmiştir. Bulgular: Tüm bileşikler arasında 1-metil-2{2"[N,Ndimetilaminokarbamoyl-tio)asetil]}benzimidazol (2b) maddesi kayda değer in vitro antikolinesteraz aktivite göstermiştir. Referans madde olarak kullanılan Donepezil ile aynı koşullarda kıyaslandığında, 2b maddesi %37 oranında inhibe ettiği görülmüştür. Sonuç: Sentezlenen sekiz yeni bileşikten sadece (1-metil-2{2"[N,Ndimetilaminokarbamoyl-tio)asetil]}benzimidazol (2b) maddesi Donepezil ile kıyaslandığında, kayda değer in vitro antikolinesteraz aktiviteye sahip olduğu tespit edilmiştir.

Anahtar Kelimeler:

Benzimidazol, Ditiokarbamat, Antikolinesteraz Aktivite

Synthesis and Biological Evaluation of Some New Benzimidazole Derivatives Bearing Dithiocarbamate Moiety as Potential Cholinesterase Inhibitors

Purpose: The synthesis of eight new benzimidazole derivatives bearing dithiocarbamate moiety and subsequently their anticholinesterase activity evaluations were aimed in this present study. Material and Method: 2-Bromoacetylbenzimidazole react with dithiocarbamate salt derivatives and the resulted compounds were elucidated by 1H NMR, mass spectral data, and elemental analyses. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) in vitro by using a modification of Ellman"s spectrophotometric method. Results: The new compound 1-methyl-2{2"[(N,Ndimethylaminothiocarbamoylthio)-acetyl]}benzimidazole (2b) can be identified as promising anticholinesterase agent in vitro due to its moderate inhibition effect, which is about 37%, when compared with standard substance Donepezil under the same experimental conditions. Conclusion: In comparing with the reference standard, among the synthesized eight new compounds the only compound namely 1-methyl-2{2"[(N,Ndimethylaminothiocarbamoyl-thio)-acetyl]}benzimidazole (2b) has a promising anticholinesterase activity.

Keywords:

Benzimidazole, Dithiocarbamate, Anticholinesterase Activity,

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Yazışma Adresi / Address for Correspondence: Dr.Usama Abu Mohsen Faculty of Pharmacy, Al-Azhar University, Department of Pharmaceutical Chemistry, Gaza, PALESTINE E-mail: usamapharmacy@gmail.com G eliş tarihi/Received on :21.03.2014
Kabul tarihi/Accepted on: 25.04.2014