2. Academic Validation
  3. 2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease

2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease

  • Eur J Med Chem. 2021 Feb 5:211:113112. doi: 10.1016/j.ejmech.2020.113112.
Eva Mezeiova 1,  Jana Janockova 1,  Rudolf Andrys 2,  Ondrej Soukup 1,  Tereza Kobrlova 1,  Lubica Muckova 3,  Jaroslav Pejchal 4,  Miriama Simunkova 5,  Jiri Handl 6,  Petra Micankova 6,  Jan Capek 6,  Tomas Rousar 6,  Martina Hrabinova 3,  Eugenie Nepovimova 2,  Jose Luis Marco-Contelles 7,  Marian Valko 8,  Jan Korabecny 9
Affiliations

Affiliations

  • 1 University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05, Hradec Kralove, Czech Republic.
  • 2 University Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03, Hradec Kralove, Czech Republic.
  • 3 University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05, Hradec Kralove, Czech Republic; University of Defence in Brno, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01, Hradec Kralove, Czech Republic.
  • 4 University of Defence in Brno, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01, Hradec Kralove, Czech Republic.
  • 5 Slovak University of Technology, Faculty of Chemical and Food Technology, Radlinskeho 9, 812 37, Bratislava, Slovakia.
  • 6 University of Pardubice, Faculty of Chemical Technology, Department of Biological and Biochemical Sciences, Studentska 573, 532 10, Pardubice, Czech Republic.
  • 7 Institute of General Organic Chemistry, Laboratory of Medicinal Chemistry, Juan de La Cierva 3, 28006, Madrid, Spain. Electronic address: jlmarco@iqog.csic.es.
  • 8 Slovak University of Technology, Faculty of Chemical and Food Technology, Radlinskeho 9, 812 37, Bratislava, Slovakia. Electronic address: marian.valko@stuba.sk.
  • 9 University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05, Hradec Kralove, Czech Republic; University of Defence in Brno, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01, Hradec Kralove, Czech Republic. Electronic address: jan.korabecny@fnhk.cz.
PMID: 33360800 DOI: 10.1016/j.ejmech.2020.113112
Abstract

Alzheimer's disease is a progressive brain disorder with characteristic symptoms and several pathological hallmarks. The concept of "one drug, one target" has not generated any new drugs since 2004. The new era of drug development in the field of AD builds upon rationally designed multi-target directed ligands that can better address the complexity of AD. Herewith, we designed ten novel derivatives of 2-propargylamino-naphthoquinone. The biological evaluation of these compounds includes inhibition of Monoamine Oxidase A/B, inhibition of amyloid-beta aggregation, radical-scavenging, and metal-chelating properties. Some of the compounds possess low cytotoxicity profile with an anti-inflammatory ability in the lipopolysaccharide-stimulated cellular model. All these features warrant their further testing in the field of AD.

Keywords

Alzheimer’s disease; Amyloid-beta; Antioxidant; Inflammation; Monoamine oxidase; Multi-target directed ligand; Naphthoquinone.

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