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Title
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New tacrin e-derived AChE/BuChE inhibitors: Synthesis and biological evaluation of 5-amino-2-p henyl-4 H -pyrano[2,3- b ]quinoline -3-carboxylates
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Type
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JournalPaper
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Keywords
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Acetylcholinesterase, Butyrylcholinesterase, Alzheimer's disease, Tacrine
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Abstract
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A series of poly-functionalized tacrine-derived compounds namely 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates were designed and synthesized as cholinesterases inhibitors. The in vitro inhibition assay against AChE and BuChE demonstrated that most of compounds had potent AChE inhibitory with reserving potential of BuChE inhibition. Among them, compound 6i bearing a 4-(3-bromophenyl) moiety showed the most potent activity against AChE/BuChE (IC50s values of 0.069 and 1.35 μM, respectively). The anti-AChE activity of 6i was five times more than that of tacrine. The SAR study revealed that chloro/bromo substituent at ortho or meta position of the 4-phenyl ring can improve the anticholinesterase activity.
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Researchers
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Alireza Foroumadi (Not In First Six Researchers), Omid Sabzevari (Not In First Six Researchers), Ali Asadipour (Not In First Six Researchers), Loghman Firoozpour (Not In First Six Researchers), Saeed Emami (Not In First Six Researchers), Farshad Homayouni Moghadam (Not In First Six Researchers), Alireza Moradi (Fifth Researcher), Mohammad Mahdavi (Fourth Researcher), Hamid Nadri (Third Researcher), Yaghoub Sarrafi (Second Researcher), Mohammad Eghtedari (First Researcher)
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