Triazole substituted metal-free,metallo-phthalocyanines and their water soluble derivatives as potential cholinesterases inhibitors: Design,synthesis and in vitro inhibition study |
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| Affiliation: | 1. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran;2. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran;3. Department of Chemistry, North Tehran Branch, Islamic Azad University, Tehran, Iran;4. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran;5. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran;6. Department of Medicinal Chemistry, School of Pharmacy, Iran University of Medical Sciences, Tehran, Iran |
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| 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 µM) and 5a showed the most effective inhibitor of BChE (IC50 = 0.1198 µM). |
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| Keywords: | Cholinesterases Inhibitors Water soluble phthalocyanine |
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