SYNTHESIS AND BIOLOGICAL EVALUATION OF MANNICH BASES OF BENZIMIDAZOLE 2 PHENOL DERIVATIVES ASANTICHOLINESTERASE AGENTS


Alpan A. S. , Sarıkaya G. , Parlar Çoşkun S. , İstanbullu H. , Alptüzün V. , Erciyas E.

1st International Gazi Pharma Symposium Series (GPSS-2015), Antalya, Türkiye, 12 - 15 Kasım 2015, ss.182

  • Basıldığı Şehir: Antalya
  • Basıldığı Ülke: Türkiye
  • Sayfa Sayısı: ss.182

Özet

Alzheimer’s disease is an age-related neurodegenative disorder which affects more than 35 million people worldwide and involves in 60-80% of the dementia cases [1], [2]. Neurotransmitter acetylcholin’s deficiency in central nervous system causes cognitive impairement in Alzheimer patients. The cholinergic approach for the therapy of this disease is using either an agonist or AChE (acetylcholinesterase) inhibitor to increase the cholinergic function [3]. In our previous study, a group of N-{2-[4-(1H-benzimidazole-2-yl)phenoxy]ethyl}substituted amine derivatives were synthesized and evaluated for their inhibitor activity against AChE [4]. Most of the compounds were exhibited good inhibition. Also we known that, an important number of studies report the activity of Mannich bases as AChE inhibitors [5]. In this study, a series of novel ‘mannich bases of 2-phenolsubstitutedbenzimidazole’ derivatives (Fig 1) were synthesized and characterized by 1 H NMR, mass spectral studies and elemental analysis. The compounds evaluated for the inhibition activity against AChE by using Ellman’s method [6]. The final compounds exhibited from moderate to good activities to the AChE enzyme compared to the standart drug.