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Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular docking of new acridine-coumarin hybrids.
Hamulakova, Slavka; Janovec, Ladislav; Soukup, Ondrej; Jun, Daniel; Kuca, Kamil.
Afiliación
  • Hamulakova S; Department of Organic Chemistry, Institute of Chemical Sciences, Faculty of Science, P. J. Safarik University, Moyzesova 11, SK-041 67 Kosice, Slovak Republic. Electronic address: slavka.hamulakova@upjs.sk.
  • Janovec L; Department of Organic Chemistry, Institute of Chemical Sciences, Faculty of Science, P. J. Safarik University, Moyzesova 11, SK-041 67 Kosice, Slovak Republic.
  • Soukup O; Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic; Department of Toxicology and Military Pharmacy, Faculty Military Helath Sciences, University of Defense, Trebesska 1575, 500 05 Hradec Kralove, Czech Republic.
  • Jun D; Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic; Department of Toxicology and Military Pharmacy, Faculty Military Helath Sciences, University of Defense, Trebesska 1575, 500 05 Hradec Kralove, Czech Republic.
  • Kuca K; Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic; Department of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanského 62, 500 03 Hradec Kralove, Czech Republic.
Int J Biol Macromol ; 104(Pt A): 333-338, 2017 Nov.
Article en En | MEDLINE | ID: mdl-28601645
ABSTRACT
A novel series of acridine-coumarin hybrids was synthesized and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The newly synthesized derivatives 9a-d have shown higher activity against human AChE (hAChE) compared with 7-MEOTA as the standard drug. Among them derivative 9b exhibited the most potent acetylcholinesterase inhibitory activity, with an IC50 value of 5.85µM compared with 7-MEOTA (IC50=15µM). Molecular modelling studies were performed to predict the binding modes of compounds 9b, 9c and 9f with hAChE/hBuChE.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Acetilcolinesterasa / Acridinas / Inhibidores de la Colinesterasa / Cumarinas / Simulación del Acoplamiento Molecular Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Int J Biol Macromol Año: 2017 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Acetilcolinesterasa / Acridinas / Inhibidores de la Colinesterasa / Cumarinas / Simulación del Acoplamiento Molecular Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Int J Biol Macromol Año: 2017 Tipo del documento: Article