Full Text Journal Articles by
Author Ondrej Soukup

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Monoterpene indole alkaloids from Vinca minor L. (Apocynaceae): Identification of new structural scaffold for treatment of Alzheimer's disease.

Rudolf Vrabec, Jana Maříková, Miroslav Ločárek, Jan Korábečný, Daniela Hulcová, Anna Hošťálková, Jiří Kuneš, Jakub Chlebek, Tomáš Kučera, Martina Hrabinová, Daniel Jun, Ondřej Soukup, Vincenza Andrisano, Jaroslav Jenčo, Marcela Šafratová, Lucie Nováková, Lubomír Opletal, Lucie Cahlíková,

One undescribed indole alkaloid together with twenty-two known compounds have been isolated from aerial parts of Vinca minor L. (Apocynaceae). The chemical structures of the isolated alkaloids were determined by a combination of MS, HRMS, 1D, and 2D NMR techniques, and by comparison with literature data. The NMR data of ... Read more >>

Phytochemistry (Phytochemistry)
[2021, 194:113017]

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Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D2 3,4-dihydroquinolin-2(1H)-one Derivatives Related to Aripiprazole.

Radomir Juza, Kristyna Stefkova, Wim Dehaen, Alena Randakova, Tomas Petrasek, Iveta Vojtechova, Tereza Kobrlova, Lenka Pulkrabkova, Lubica Muckova, Marko Mecava, Lukas Prchal, Eva Mezeiova, Kamil Musilek, Ondrej Soukup, Jan Korabecny,

In this pilot study, a series of new 3,4-dihydroquinolin-2(1<i>H</i>)-one derivatives as potential dopamine receptor D<sub>2</sub> (D<sub>2</sub>R) modulators were synthesized and evaluated in vitro. The preliminary structure-activity relationship disclosed that compound <b>5e</b> exhibited the highest D<sub>2</sub>R affinity among the newly synthesized compounds. In addition, <b>5e</b> showed a very low cytotoxic profile ... Read more >>

Biomolecules (Biomolecules)
[2021, 11(9):]

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Amaryllidaceae Alkaloids of Norbelladine-Type as Inspiration for Development of Highly Selective Butyrylcholinesterase Inhibitors: Synthesis, Biological Activity Evaluation, and Docking Studies.

Abdullah Al Mamun, Filip Pidaný, Daniela Hulcová, Jana Maříková, Tomáš Kučera, Monika Schmidt, Maria Carmen Catapano, Martina Hrabinová, Daniel Jun, Lubica Múčková, Jiří Kuneš, Jiří Janoušek, Rudolf Andrýs, Lucie Nováková, Rozálie Peřinová, Negar Maafi, Ondřej Soukup, Jan Korábečný, Lucie Cahlíková,

Alzheimer's disease (AD) is a multifactorial neurodegenerative condition of the central nervous system (CNS) that is currently treated by cholinesterase inhibitors and the <i>N</i>-methyl-d-aspartate receptor antagonist, memantine. Emerging evidence strongly supports the relevance of targeting butyrylcholinesterase (BuChE) in the more advanced stages of AD. Within this study, we have generated ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2021, 22(15):]

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Cholinesterase Research.

Jan Korabecny, Ondrej Soukup,

Cholinesterases are fundamental players in the peripheral and central nervous systems [...]. ... Read more >>

Biomolecules (Biomolecules)
[2021, 11(8):]

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Discovery of sustainable drugs for Alzheimer's disease: cardanol-derived cholinesterase inhibitors with antioxidant and anti-amyloid properties.

Giselle de Andrade Ramos, Andressa Souza de Oliveira, Manuela Bartolini, Marina Naldi, Irene Liparulo, Christian Bergamini, Elisa Uliassi, Ling Wu, Paul E Fraser, Monica Abreu, Alessandra Sofia Kiametis, Ricardo Gargano, Edilberto Rocha Silveira, Guilherme D Brand, Lukas Prchal, Ondřej Soukup, Jan Korábečný, Maria Laura Bolognesi, Luiz Antonio Soares Romeiro,

As part of our efforts to develop sustainable drugs for Alzheimer's disease (AD), we have been focusing on the inexpensive and largely available cashew nut shell liquid (CNSL) as a starting material for the identification of new acetylcholinesterase (AChE) inhibitors. Herein, we decided to investigate whether cardanol, a phenolic CNSL ... Read more >>

RSC Med Chem (RSC medicinal chemistry)
[2021, 12(7):1154-1163]

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Amiridine-piperazine hybrids as cholinesterase inhibitors and potential multitarget agents for Alzheimer's disease treatment.

Galina F Makhaeva, Sofya V Lushchekina, Nadezhda V Kovaleva, Tatiana Yu Astakhova, Natalia P Boltneva, Elena V Rudakova, Olga G Serebryakova, Alexey N Proshin, Igor V Serkov, Tatiana P Trofimova, Victor A Tafeenko, Eugene V Radchenko, Vladimir A Palyulin, Vladimir P Fisenko, Jan Korábečný, Ondrej Soukup, Rudy J Richardson,

We synthesized eleven new amiridine-piperazine hybrids 5a-j and 7 as potential multifunctional agents for Alzheimer's disease (AD) treatment by reacting N-chloroacetylamiridine with piperazines. The compounds displayed mixed-type reversible inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Conjugates were moderate inhibitors of equine and human BChE with negligible fluctuation in anti-BChE activity, ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 112:104974]

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Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors.

Lukas Gorecki, Anna Misiachna, Jiri Damborsky, Rafael Dolezal, Jan Korabecny, Lada Cejkova, Kristina Hakenova, Marketa Chvojkova, Jana Zdarova Karasova, Lukas Prchal, Martin Novak, Marharyta Kolcheva, Stepan Kortus, Karel Vales, Martin Horak, Ondrej Soukup,

Tacrine is a classic drug whose efficacy against neurodegenerative diseases is still shrouded in mystery. It seems that besides its inhibitory effect on cholinesterases, the clinical benefit is co-determined by NMDAR-antagonizing activity. Our previous data showed that the direct inhibitory effect of tacrine, as well as its 7-methoxy derivative (7-MEOTA), ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 219:113434]

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Phenothiazine-Tacrine Heterodimers: Pursuing Multitarget Directed Approach in Alzheimer's Disease.

Lukas Gorecki, Elisa Uliassi, Manuela Bartolini, Jana Janockova, Martina Hrabinova, Vendula Hepnarova, Lukas Prchal, Lubica Muckova, Jaroslav Pejchal, Jana Z Karasova, Eva Mezeiova, Marketa Benkova, Tereza Kobrlova, Ondrej Soukup, Sabrina Petralla, Barbara Monti, Jan Korabecny, Maria Laura Bolognesi,

Since 2002, no clinical candidate against Alzheimer's disease has reached the market; hence, an effective therapy is urgently needed. We followed the so-called "multitarget directed ligand" approach and designed 36 novel tacrine-phenothiazine heterodimers which were <i>in vitro</i> evaluated for their anticholinesterase properties. The assessment of the structure-activity relationships of such ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2021, 12(9):1698-1715]

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Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.

Eva Mezeiova, Martina Hrabinova, Vendula Hepnarova, Daniel Jun, Jana Janockova, Lubica Muckova, Lukas Prchal, Zdena Kristofikova, Tomas Kucera, Lukas Gorecki, Katarina Chalupova, Jiri Kunes, Jana Hroudova, Ondrej Soukup, Jan Korabecny,

The search for novel and effective therapeutics for Alzheimer's disease (AD) is the main quest that remains to be resolved. The goal is to find a disease-modifying agent able to confront the multifactorial nature of the disease positively. Herewith, a family of huprineY-tryptophan heterodimers was prepared, resulting in inhibition of ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2021, 43:128100]

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Design and synthesis of novel tacrine-indole hybrids as potential multitarget-directed ligands for the treatment of Alzheimer's disease.

Slavka Hamulakova, Zuzana Kudlickova, Ladislav Janovec, Roman Mezencev, Zachery J Deckner, Yury O Chernoff, Jana Janockova, Veronika Ihnatova, Petr Bzonek, Nikola Novakova, Vendula Hepnarova, Martina Hrabinova, Daniel Jun, Jan Korabecny, Ondrej Soukup, Kamil Kuca,

The authors report on the synthesis and biological evaluation of new compounds whose structure combines tacrine and indole moieties. Tacrine-indole heterodimers were designed to inhibit cholinesterases and β-amyloid formation, and to cross the blood-brain barrier. The most potent new acetylcholinesterase inhibitors were compounds <b>3c</b> and <b>4d</b> (IC<sub>50</sub> = 25 and 39 nM, respectively). ... Read more >>

Future Med Chem (Future medicinal chemistry)
[2021, 13(9):785-804]

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(±)-BIGI-3h: Pentatarget-Directed Ligand combining Cholinesterase, Monoamine Oxidase, and Glycogen Synthase Kinase 3β Inhibition with Calcium Channel Antagonism and Antiaggregating Properties for Alzheimer's Disease.

Lhassane Ismaili, Julie Monnin, Adeline Etievant, Raquel L Arribas, Lucía Viejo, Bernard Refouvelet, Ondrej Soukup, Jana Janockova, Vendula Hepnarova, Jan Korabecny, Tomas Kucera, Daniel Jun, Rudolf Andrys, Kamil Musilek, Aurelie Baguet, Eva M García-Frutos, Angela De Simone, Vincenza Andrisano, Manuela Bartolini, Cristóbal de Los Ríos, José Marco-Contelles, Emmanuel Haffen,

Multitarget-directed ligands (MTDLs) are considered a promising therapeutic strategy to address the multifactorial nature of Alzheimer's disease (AD). Novel MTDLs have been designed as inhibitors of human acetylcholinesterases/butyrylcholinesterases, monoamine oxidase A/B, and glycogen synthase kinase 3β and as calcium channel antagonists via the Biginelli multicomponent reaction. Among these MTDLs, (±)<b>-BIGI-3h</b> ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2021, 12(8):1328-1342]

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Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.

Michele Rossi, Michela Freschi, Luciana de Camargo Nascente, Alessandra Salerno, Sarah de Melo Viana Teixeira, Florian Nachon, Fabien Chantegreil, Ondrej Soukup, Lukáš Prchal, Marco Malaguti, Christian Bergamini, Manuela Bartolini, Cristina Angeloni, Silvana Hrelia, Luiz Antonio Soares Romeiro, Maria Laura Bolognesi,

The multifactorial nature of Alzheimer's disease (AD) is a reason for the lack of effective drugs as well as a basis for the development of "multi-target-directed ligands" (MTDLs). As cases increase in developing countries, there is a need of new drugs that are not only effective but also accessible. With ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2021, 64(8):4972-4990]

Cited: 2 times

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Synthesis of New Biscoumarin Derivatives, In Vitro Cholinesterase Inhibition, Molecular Modelling and Antiproliferative Effect in A549 Human Lung Carcinoma Cells.

Monika Hudáčová, Slávka Hamuľaková, Eva Konkoľová, Rastislav Jendželovský, Jana Vargová, Juraj Ševc, Peter Fedoročko, Ondrej Soukup, Jana Janočková, Veronika Ihnatova, Tomáš Kučera, Petr Bzonek, Nikola Novakova, Daniel Jun, Lucie Junova, Jan Korábečný, Kamil Kuča, Mária Kožurková,

A series of novel C4-C7-tethered biscoumarin derivatives (<b>12a</b>-<b>e</b>) linked through piperazine moiety was designed, synthesized, and evaluated biological/therapeutic potential. Biscoumarin <b>12d</b> was found to be the most effective inhibitor of both acetylcholinesterase (AChE, IC<sub>50</sub> = 6.30 µM) and butyrylcholinesterase (BChE, IC<sub>50</sub> = 49 µM). Detailed molecular modelling studies compared the ... Read more >>

Int J Mol Sci (International journal of molecular sciences)
[2021, 22(8):]

Cited: 1 time

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Development of versatile and potent monoquaternary reactivators of acetylcholinesterase.

Lukas Gorecki, Vendula Hepnarova, Jana Zdarova Karasova, Martina Hrabinova, Charlotte Courageux, José Dias, Tomas Kucera, Tereza Kobrlova, Lubica Muckova, Lukas Prchal, David Malinak, Daniel Jun, Kamil Musilek, Franz Worek, Florian Nachon, Ondrej Soukup, Jan Korabecny,

To date, the only treatments developed for poisoning by organophosphorus compounds, the most toxic chemical weapons of mass destruction, have exhibited limited efficacy and versatility. The available causal antidotes are based on reactivation of the enzyme acetylcholinesterase (AChE), which is rapidly and pseudo-irreversibly inhibited by these agents. In this study, ... Read more >>

Arch Toxicol (Archives of toxicology)
[2021, 95(3):985-1001]

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7-phenoxytacrine is a dually acting drug with neuroprotective efficacy in vivo.

Martina Kaniakova, Jan Korabecny, Kristina Holubova, Lenka Kleteckova, Marketa Chvojkova, Kristina Hakenova, Lukas Prchal, Martin Novak, Rafael Dolezal, Vendula Hepnarova, Barbora Svobodova, Tomas Kucera, Katarina Lichnerova, Barbora Krausova, Martin Horak, Karel Vales, Ondrej Soukup,

N-methyl-D-aspartaterecepro receptor (NMDARs) are a subclass of glutamate receptors, which play an essential role in excitatory neurotransmission, but their excessive overactivation by glutamate leads to excitotoxicity. NMDARs are hence a valid pharmacological target for the treatment of neurodegenerative disorders; however, novel drugs targeting NMDARs are often associated with specific psychotic ... Read more >>

Biochem Pharmacol (Biochemical pharmacology)
[2021, 186:114460]

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Pursuing the Complexity of Alzheimer's Disease: Discovery of Fluoren-9-Amines as Selective Butyrylcholinesterase Inhibitors and N-Methyl-d-Aspartate Receptor Antagonists.

Jan Konecny, Anna Misiachna, Martina Hrabinova, Lenka Pulkrabkova, Marketa Benkova, Lukas Prchal, Tomas Kucera, Tereza Kobrlova, Vladimir Finger, Marharyta Kolcheva, Stepan Kortus, Daniel Jun, Marian Valko, Martin Horak, Ondrej Soukup, Jan Korabecny,

Alzheimer's disease (AD) is a complex disorder with unknown etiology. Currently, only symptomatic therapy of AD is available, comprising cholinesterase inhibitors and <i>N</i>-methyl-d-aspartate (NMDA) receptor antagonists. Drugs targeting only one pathological condition have generated only limited efficacy. Thus, combining two or more therapeutic interventions into one molecule is believed to ... Read more >>

Biomolecules (Biomolecules)
[2020, 11(1):]

Cited: 2 times

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

Eva Mezeiova, Jana Janockova, Rudolf Andrys, Ondrej Soukup, Tereza Kobrlova, Lubica Muckova, Jaroslav Pejchal, Miriama Simunkova, Jiri Handl, Petra Micankova, Jan Capek, Tomas Rousar, Martina Hrabinova, Eugenie Nepovimova, Jose Luis Marco-Contelles, Marian Valko, Jan Korabecny,

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 ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2021, 211:113112]

Cited: 1 time

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Tacrine - Benzothiazoles: Novel class of potential multitarget anti-Alzheimeŕs drugs dealing with cholinergic, amyloid and mitochondrial systems.

Eugenie Nepovimova, Lucie Svobodova, Rafael Dolezal, Vendula Hepnarova, Lucie Junova, Daniel Jun, Jan Korabecny, Tomas Kucera, Zuzana Gazova, Katarina Motykova, Jana Kubackova, Zuzana Bednarikova, Jana Janockova, Catarina Jesus, Luisa Cortes, Joao Pina, Danijela Rostohar, Carlos Serpa, Ondrej Soukup, Laura Aitken, Rebecca E Hughes, Kamil Musilek, Lubica Muckova, Petr Jost, Marketa Chvojkova, Karel Vales, Martin Valis, Zofia Chrienova, Katarina Chalupova, Kamil Kuca,

A series of tacrine - benzothiazole hybrids incorporate inhibitors of acetylcholinesterase (AChE), amyloid β (Aβ) aggregation and mitochondrial enzyme ABAD, whose interaction with Aβ leads to mitochondrial dysfunction, into a single molecule. In vitro, several of 25 final compounds exerted excellent anti-AChE properties and interesting capabilities to block Aβ aggregation. ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 107:104596]

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Is It the Twilight of BACE1 Inhibitors?

Martina Hrabinova, Jaroslav Pejchal, Tomas Kucera, Daniel Jun, Monika Schmidt, Ondrej Soukup,

β-secretase (BACE1) has been regarded as a prime target for the development of amyloid beta (Aβ) lowering drugs in the therapy of Alzheimer´s disease (AD). Although the enzyme was discovered in 1991 and helped to formulate the Aβ hypothesis as one of the very important features of AD etiopathogenesis, progress ... Read more >>

Curr Neuropharmacol (Current neuropharmacology)
[2021, 19(1):61-77]

Cited: 1 time

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α-Linolenic Acid-Valproic Acid Conjugates: Toward Single-Molecule Polypharmacology for Multiple Sclerosis.

Michele Rossi, Sabrina Petralla, Michele Protti, Monica Baiula, Tereza Kobrlova, Ondrej Soukup, Santi Mario Spampinato, Laura Mercolini, Barbara Monti, Maria Laura Bolognesi,

Multiple sclerosis (MS) is a complex inflammatory, degenerative, and demyelinating disease of the central nervous system. Although treatments exist, MS cannot be cured by available drugs, which primarily target neuroinflammation. Thus, it is feasible that a well concerted polypharmacological approach able to act at multiple points within the intricate network ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2020, 11(12):2406-2413]

Cited: 2 times

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Effect of P-glycoprotein on the availability of oxime reactivators in the brain.

Tereza Kobrlova, Ondrej Soukup,

The ability to overcome cellular barriers in the body is crucial for efficient delivery of drugs to the target where intervention is needed. For drugs acting in the brain it is essential to overcome the blood-brain barrier (BBB). Such drugs include antidotes for the treatment of organophosphate poisoning, a current ... Read more >>

Toxicology (Toxicology)
[2020, 443:152541]

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Turning Donepezil into a Multi-Target-Directed Ligand through a Merging Strategy.

Rosaria Perone, Claudia Albertini, Elisa Uliassi, Flaminia Di Pietri, Pedro de Sena Murteira Pinheiro, Sabrina Petralla, Nicola Rizzardi, Romana Fato, Lenka Pulkrabkova, Ondrej Soukup, Anna Tramarin, Manuela Bartolini, Maria Laura Bolognesi,

Thanks to the widespread use and safety profile of donepezil (1) in the treatment of Alzheimer's disease (AD), one of the most widely adopted multi-target-directed ligand (MTDL) design strategies is to modify its molecular structure by linking a second fragment carrying an additional AD-relevant biological property. Herein, supported by a ... Read more >>

ChemMedChem (ChemMedChem)
[2021, 16(1):187-198]

Cited: 1 time

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The wide-spectrum antimicrobial effect of novel N-alkyl monoquaternary ammonium salts and their mixtures; the QSAR study against bacteria.

Ondrej Soukup, Marketa Benkova, Rafael Dolezal, Radek Sleha, David Malinak, Sarka Salajkova, Aneta Markova, Michaela Hympanova, Lukas Prchal, Lenka Ryskova, Lenka Hobzova, Kristina Sepčić, Nina Gunde-Cimerman, Jan Korabecny, Daniel Jun, Vanda Bostikova, Pavel Bostik, Jan Marek,

Quaternary ammonium salts (QASs) have been widely used for disinfection purposes because of their low price, high efficacy and low human toxicity for decades. However, precise mechanisms of action nor the powerful versatile agent against all antimicrobial species are known. In this study we have prepared 43 novel N-alkyl monoquaternary ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2020, 206:112584]

Cited: 3 times

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From orexin receptor agonist YNT-185 to novel antagonists with drug-like properties for the treatment of insomnia.

Eva Mezeiova, Jana Janockova, Jan Konecny, Tereza Kobrlova, Marketa Benkova, Rafael Dolezal, Lukas Prchal, Jana Karasova-Zdarova, Ondrej Soukup, Jan Korabecny,

YNT-185 is the first known small molecule acting as orexin 2 receptor (OX<sub>2</sub>R) agonist with implication to narcolepsy treatment, served as a template scaffold in generating a small set of seven compounds with predictive affinity to OX<sub>2</sub>R. The design of the new small molecules was driven mostly by improving physicochemical ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2020, 103:104179]

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Discovery of novel berberine derivatives with balanced cholinesterase and prolyl oligopeptidase inhibition profile.

Katerina Sobolova, Martina Hrabinova, Vendula Hepnarova, Tomas Kucera, Tereza Kobrlova, Marketa Benkova, Jana Janockova, Rafael Dolezal, Lukas Prchal, Ondrej Benek, Eva Mezeiova, Daniel Jun, Ondrej Soukup, Jan Korabecny,

Berberine, a naturally occurring compound, possesses an interesting multipotent pharmacological profile potentially applicable for Alzheimer's disease (AD) treatment. In this study, a series of novel 22 berberine derivatives was developed and tested in vitro. Berberine core was substituted at position 9-O of its aromatic ring region. All the hybrids under the ... Read more >>

Eur J Med Chem (European journal of medicinal chemistry)
[2020, 203:112593]

Cited: 4 times

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