2-PROPARGAYLAMINO-NAPHTHOQUINONE DERIVATIVES AS MULTIPOTENT AGENTS FOR THE TREATMENT OF ALZHEIMER’S DISEASE

MMSL 2022, 91(88):57

2-PROPARGAYLAMINO-NAPHTHOQUINONE DERIVATIVES AS MULTIPOTENT AGENTS FOR THE TREATMENT OF ALZHEIMER’S DISEASEMeeting abstracts

Eva Mezeiova¹, Jan Konecny¹, Jana Janockova¹, Rudolf Andrys², Ondrej Soukup¹, Tereza Kobrlova¹, Lubica Muckova^1,3, Jaroslav Pejchal³, Miriama Simunkova⁴, Jiri Handl⁵, Petra Micankova⁵, Jan Capek⁵, Tomas Rousar⁵, Martina Hrabinova^1,3, Eugenie Nepovimova², Jose Luis Marco-Contelles⁶, Marian Valko⁴, Jan Korabecny^1,3: ¹ University Hospital Hradec Kralove, Biomedical Research Centre, Sokolska 581, 500 05 Hradec Kralove, The Czech Republic; ² University Hradec Kralove, Faculty of Science, Department of chemistry, Rokitanskeho 62, 500 03 Hradec Kralove, The Czech Republic; ³ University of Defence in Brno, Faculty of Military Health Sciences, Department of Toxicology and Military Pharmacy, Trebesska 1575, 500 01 Hradec Kralove, The Czech Republic; ⁴ Slovak University of Technology, Faculty of Chemical and Food Technology, Radlinskeho 9, 812 37 Bratislava, Slovakia; ⁵ University of Pardubice, Faculty of Chemical Technology, Department of Biological Sciencies, Studentska 573, 532 10 Pardubice, The Czech Republic; ⁶ Institute of General Organic Chemistry, Laboratory of Medicinal Chemistry, Juan de La Cierva 3, 28006, Madrid, Spain

Alzheimer’s disease (AD) 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 (1). 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 (2).

Keywords: Alzheimer’s disease; naphthoquinone; multi-target directed ligand; amyloid-beta; monoamine oxidase

Published: June 20, 2022 Show citation

Mezeiova, E., Konecny, J., Janockova, J., Andrys, R., Soukup, O., Kobrlova, T., ... Korabecny, J. (2022). 2-PROPARGAYLAMINO-NAPHTHOQUINONE DERIVATIVES AS MULTIPOTENT AGENTS FOR THE TREATMENT OF ALZHEIMER’S DISEASE. MMSL, 91(Suppl.1), 57

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