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

E. Mezeiova, J. Janockova, R. Andrys, O. Soukup, T. Kobrlova, L. Muckova, J. Pejchal, M. Simunkova, J. Handl, P. Micankova, J. Capek, T. Rousar, M. Hrabinova, E. Nepovimova, JL. Marco-Contelles, M. Valko, J. Korabecny

. 2021 ; 211 (-) : 113112. [pub] 20201218

Language English Country France

Document type Journal Article

Persistent link   https://www.medvik.cz/link/bmc21019274

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.

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$a 2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease / $c E. Mezeiova, J. Janockova, R. Andrys, O. Soukup, T. Kobrlova, L. Muckova, J. Pejchal, M. Simunkova, J. Handl, P. Micankova, J. Capek, T. Rousar, M. Hrabinova, E. Nepovimova, JL. Marco-Contelles, M. Valko, J. Korabecny
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$a 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.
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$a Janockova, Jana $u University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05, Hradec Kralove, Czech Republic
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$a Andrys, Rudolf $u University Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03, Hradec Kralove, Czech Republic
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$a Soukup, Ondrej $u University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05, Hradec Kralove, Czech Republic
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$a Kobrlová, Tereza, $u University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05, Hradec Kralove, Czech Republic $d 1991- $7 xx0277928
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$a Muckova, Lubica $u University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05, Hradec Kralove, Czech Republic; University of Defence in Brno, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01, Hradec Kralove, Czech Republic
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$a Pejchal, Jaroslav $u University of Defence in Brno, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01, Hradec Kralove, Czech Republic
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$a Simunkova, Miriama $u Slovak University of Technology, Faculty of Chemical and Food Technology, Radlinskeho 9, 812 37, Bratislava, Slovakia
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$a Handl, Jiri $u University of Pardubice, Faculty of Chemical Technology, Department of Biological and Biochemical Sciences, Studentska 573, 532 10, Pardubice, Czech Republic
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$a Micankova, Petra $u University of Pardubice, Faculty of Chemical Technology, Department of Biological and Biochemical Sciences, Studentska 573, 532 10, Pardubice, Czech Republic
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$a Capek, Jan $u University of Pardubice, Faculty of Chemical Technology, Department of Biological and Biochemical Sciences, Studentska 573, 532 10, Pardubice, Czech Republic
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$a Rousar, Tomas $u University of Pardubice, Faculty of Chemical Technology, Department of Biological and Biochemical Sciences, Studentska 573, 532 10, Pardubice, Czech Republic
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$a Hrabinova, Martina $u University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05, Hradec Kralove, Czech Republic; University of Defence in Brno, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01, Hradec Kralove, Czech Republic
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$a Nepovimova, Eugenie $u University Hradec Kralove, Faculty of Science, Department of Chemistry, Rokitanskeho 62, 500 03, Hradec Kralove, Czech Republic
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$a Marco-Contelles, Jose Luis $u Institute of General Organic Chemistry, Laboratory of Medicinal Chemistry, Juan de La Cierva 3, 28006, Madrid, Spain. Electronic address: jlmarco@iqog.csic.es
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$a Valko, Marian $u Slovak University of Technology, Faculty of Chemical and Food Technology, Radlinskeho 9, 812 37, Bratislava, Slovakia. Electronic address: marian.valko@stuba.sk
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$a Korabecny, Jan $u 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
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