Pharmacological and Toxicological Screening of Novel Benzimidazole-Morpholine Derivatives as Dual-Acting Inhibitors

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CAN N. Ö., ACAR ÇEVİK U., SAĞLIK B. N., ÖZKAY Y., ATLI EKLİOĞLU Ö., BAYSAL M., ...Daha Fazla

MOLECULES, cilt.22, sa.8, 2017 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 22 Sayı: 8
  • Basım Tarihi: 2017
  • Doi Numarası: 10.3390/molecules22081374
  • Dergi Adı: MOLECULES
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Anahtar Kelimeler: benzimidazoles, morpholines, AChE, MAO, COX, MONOAMINE-OXIDASE-B, ANTIMICROBIAL ACTIVITY, BIOLOGICAL EVALUATION, AGENTS, DESIGN, BEARING, MOIETY, ASSAY
  • Anadolu Üniversitesi Adresli: Evet

Özet

The aim of this study was to investigate acetylcholinesterase (AChE), monoamine oxidase A (MAO-A), monoamine oxidase B (MAO-B), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme inhibitory, and antimicrobial activities of a new series of 2-(4-substituted phenyl)-1-[2-(morpholin-4-yl)ethyl]-1H-benzimidazole derivatives, for their possible use as multi-action therapeutic agents. Target compounds (n = 15) were synthesized under microwave irradiation conditions in two steps, and their structures were elucidated by FT-IR, H-1-NMR, C-13-NMR and high resolution mass spectroscopic analyses. Pharmacological screening studies revealed that two of the compounds (2b and 2j) have inhibitory potential on both COX-1 and COX-2 enzymes. In addition, cytotoxic and genotoxic properties of the compounds 2b, 2j and 2m were investigated via the well-known MTT and Ames tests, which revealed that the mentioned compounds are non-cytotoxic and non-genotoxic. As a concise conclusion, two novel compounds were characterized as potential candidates for treatment of frequently encountered inflammatory diseases.