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Synthesis and Biological Evaluation of Novel Tacrine Derivatives and Tacrine–Coumarin Hybrids as Cholinesterase Inhibitors

J Med Chem. 2014 Aug 28;57(16):7073-84. doi: 10.1021/jm5008648. Epub 2014 Aug 12.Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.Hamulakova S1, Janovec L, Hrabinova M, Spilovska K, Korabecny J, Kristian P, Kuca K, Imrich J.Author information1Institute of Chemistry, Faculty of Science, P. J. Safarik University , SK-041 67 Kosice, Slovak Republic.AbstractA series of novel tacrine derivatives and tacrine-coumarin heterodimers were designed, synthesized, and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Of these compounds, tacrine-coumarin heterodimer 7c and tacrine derivative 6b were found to be the most potent inhibitors of human AChE (hAChE), demonstrating IC50 values of 0.0154 and 0.0263 μM. Ligands 6b, 6c, and 7c exhibited the highest levels of inhibitory activity against human BuChE (hBuChE), demonstrating IC50 values that range from 0.228 to 0.328 μM. Docking studies were performed in order to predict the binding modes of compounds 6b and 7c with hAChE/hBuChE.PMID: 25089370 DOI: 10.1021/jm5008648 [Indexed for MEDLINE] SharePublication types, MeSH terms, Substances, Grant supportPublication typesResearch Support, N.I.H., ExtramuralResearch Support, Non-U.S. Gov'tMeSH termsAcetylcholinesterase/chemistryAcetylcholinesterase/metabolismButyrylcholinesterase/chemistryButyrylcholinesterase/metabolismChemistry Techniques, SyntheticCholinesterase Inhibitors/chemical synthesisCholinesterase Inhibitors/chemistry*Cholinesterase Inhibitors/pharmacology*Coumarins/chemistry*Drug Evaluation, Preclinical/methodsHumansInhibitory Concentration 50Molecular Docking SimulationStructure-Activity RelationshipTacrine/chemistry*SubstancesCholinesterase InhibitorsCoumarinsTacrinecoumarinAcetylcholinesteraseButyrylcholinesteraseGrant supportP41 RR-01081/RR/NCRR NIH HHS/United StatesLinkOut - more resourcesFull Text SourcesAmerican Chemical SocietyOther Literature SourcesCited by Patents in - The LensChemical InformationBindingDBMiscellaneousCOUMARIN - Hazardous Substances Data Bank

ترکیب و ارزیابی بیولوژیکی مشتقات Tacrine جدید و مشتقات Tacrine - Coumarin Hybrids بعنوان مهار کننده‌های Cholinesterase

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