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, vol.90, 2019 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 90
  • Publication Date: 2019
  • Doi Number: 10.1016/j.bioorg.2019.103100
  • Journal Name: BIOORGANIC CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Keywords: Cholinesterases, Inhibitors, Water soluble phthalocyanine, ACETYLCHOLINESTERASE, BUTYRYLCHOLINESTERASE, ACTIVATION
  • Recep Tayyip Erdoğan University Affiliated: Yes

Abstract

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).