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

[Display omitted] •Synthesis of novel metal-free and metallo phthalocyanines.•Synthesis of novel water soluble phthalocyanine.•Acetylcholinesterase inhibition of phthalocyanines.•Butyrylcholinesterase inhibition of phthalocyanines. In this study, 1,2,3-triazole substituted metal-free and metallo pht...

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Bibliographic Details
Published in:Bioorganic chemistry 2019-09, Vol.90, p.103100-103100, Article 103100
Main Authors: Arslan, Tayfun, Çakır, Nezaket, Keleş, Turgut, Biyiklioglu, Zekeriya, Senturk, Murat
Format: Article
Language:English
Subjects:
Cholinesterases
Inhibitors
Water soluble phthalocyanine
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Summary:[Display omitted] •Synthesis of novel metal-free and metallo phthalocyanines.•Synthesis of novel water soluble phthalocyanine.•Acetylcholinesterase inhibition of phthalocyanines.•Butyrylcholinesterase inhibition of phthalocyanines. 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 µM) and 5a showed the most effective inhibitor of BChE (IC50 = 0.1198 µM).
ISSN:0045-2068
1090-2120
DOI:10.1016/j.bioorg.2019.103100