Triazole substituted metal-free, metallo-phthalocyanines and their water soluble derivatives as potential cholinesterases inhibitors: Design, synthesis and in vitro inhibition study

Arslan T., Cakir N., Keles T., YIKLIOGLU Z. B., Senturk M.

BIOORGANIC CHEMISTRY, cilt.90, 2019 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 90
  • Basım Tarihi: 2019
  • Doi Numarası: 10.1016/j.bioorg.2019.103100
  • Dergi Adı: BIOORGANIC CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Anahtar Kelimeler: Cholinesterases, Inhibitors, Water soluble phthalocyanine, ACETYLCHOLINESTERASE, BUTYRYLCHOLINESTERASE, ACTIVATION
  • Recep Tayyip Erdoğan Üniversitesi Adresli: Evet

Özet

In this study, 1,2,3-triazole substituted metal-free and metallo phthalocyanines (4, 5, 6) and their water soluble derivatives (4a, 5a, 6a) were designed, synthesized for the first time and tested in vitro on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Most phthalocyanines exhibited good inhibitory activities on these enzymes. Among the six phthalocyanines and starting compounds, 4a showed the most interesting profile as a submicromolar selective inhibitor of AChE (IC50 = 0.040 mu M) and 5a showed the most effective inhibitor of BChE (IC50 = 0.1198 mu M).