Search results for: Grzegorz Kazek

Items from 1 to 19 out of 19 results

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ANALGESIC AND ANTI-INFLAMMATORY ACTIVITY OF NEW ANALOGUES OF HC-030031: A TRPA1 CHANNEL ANTAGONIST

Adrian Bryła, Marietta Ślusarczyk, Małgorzata Zygmunt, Grażyna Chłoń-Rzepa, more

Acta Poloniae Pharmaceutica - Drug Research > 2020 > 77 > 1 > 113-119

One of our study direction is research in the group of compounds affecting the TRPA1 ion channel which can perform an important function in pain (including neuropathic pain) and inflammation for example in asthma and other chronic respiratory diseases. The aim of this study was to evaluate the analgesic and anti-inflammatory activity of two analogues of HC-030031 analogues belonging to nitrogen derivatives...

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Tridentate hydrazido-hydrazones vanadium complexes. Synthesis, properties and biological activity

Janusz Szklarzewicz, Anna Jurowska, Maciej Hodorowicz, Dariusz Matoga, more

Science, Technology and Innovation > 2019 > Vol. 4, no. 1 > 9--20

Nine new vanadium complexes, with tridentate Schiff base ligand based on 3,5-di-tertbutyl-2-hydroxybenzaldehyde and different hydrazides, are described and characterized. The X-ray crystal structure of complex 8 shows distorted octahedral geometry of vanadium, with ONO ligand in equatorial position. The tridentate Schiff base ligand forms six membered and five-membered chelate rings at the V(V) acceptor...

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Potentiation of adipogenesis and insulinomimetic effects of a novel vanadium complex (N′-[(E)-(5-bromo-2oxophenyl)methylidene]-4methoxybenzohydrazide)oxido(1,10phenanthroline)vanadium(IV) in 3T3-L1 cells

Grzegorz Kazek, Monika Głuch-Lutwin, Barbara Mordyl, Elżbieta Menaszek, more

Science, Technology and Innovation > 2019 > Vol. 4, no. 1 > 55--62

Recent research on the action of vanadium compounds shows its important effect on adipogenesis processes and adipocyte function. On the basis of previous screening tests in cellular models, the novel vanadium complex (N′-[(E)-(5-bromo-2-oxophenyl)methylidene]4-methoxybenzohydrazide)oxido(1,10-phenanthroline)vanadium(IV) was selected for this study. This complex exhibits potent inhibition of tyrosine...

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Cell-based screening for identification of novel vanadium complexes with multidirectional activity relative to cells associated with metabolic disorders

Grzegorz Kazek, Monika Głuch-Lutwin, Barbara Modryl, Elżbieta Menaszek, more

Science, Technology and Innovation > 2019 > Vol. 4, no. 1 > 47--54

In this study, 110 newly synthesized vanadium complexes from different structural groups were screened in three cell-based models representing the main target tissues for anti-diabetic drugs. In glucose utilization in C2C12 myocyte experiments, 93% of vanadium complexes were shown to have equal or greater activity than bis(maltolato)oxovanadium(IV) (BMOV), the methyl analog of bis(ethylmaltolato)oxovanadium(IV)...

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Anti-aggregation effect of aroxyalkyl derivatives of 2-methoxyphenylpiperazine is due to their 5-HT2A and α2-adrenoceptor antagonistic properties. A comparison with ketanserin, sarpogrelate, prazosin, yohimbine and ARC239

Monika Kubacka, Grzegorz Kazek, Magdalena Kotańska, Barbara Filipek, more

European Journal of Pharmacology > 2018 > 818 > C > 263-270

Serotonin (5-HT) and adrenaline acting at platelet 5-HT_2A-serotoninergic and α₂-adrenergic receptors are involved in platelet aggregation. We have evaluated the antagonistic potency at 5-HT_2A, α_2A–, and α_2B-adrenoceptors as well as an anti-aggregation effect of aroxyalkyl derivatives of 2-methoxyphenylpiperazine and compared them with ketanserin, sarpogrelate, prazosin, yohimbine and ARC239 (2-[2-[4-(o-methoxyphenyl)-piperazin-1-yl]-ethyl]-4,4-dimethyl-1,3-(2H,4H)-isoquinolindione)...

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Wybrane czynniki ryzyka schizofrenii: pomiędzy różnorodnością modeli etiologicznych a psychiatrią spersonalizowaną

Natalia Śmierciak, Wirginia Krzyściak, Marta Szwajca, Grzegorz Kazek, more

Psychiatria i Psychologia Kliniczna > 2018 > 18 > 4 > 388–398

Schizofrenia należy do coraz poważniejszych problemów medycznych i społecznych. Pomimo postępu w farmakoterapii i innych formach terapii psychoz pozostaje ona zaburzeniem o chronicznym i degradującym przebiegu. Kilka dekad badań nad jej uwarunkowaniami nie przyniosło odkrycia etiologii choroby. Potwierdzone w badaniach i zweryfikowane w praktyce klinicznej hipotezy nie tłumaczą przyczyn jej powstawania...

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Aminoalkyl Derivatives of 8‐Alkoxypurine‐2,6‐diones: Multifunctional 5‐HT_1A/5‐HT₇ Receptor Ligands and PDE Inhibitors with Antidepressant Activity

Grażyna Chłoń‐Rzepa, Agnieszka Zagórska, Paweł Żmudzki, Adam Bucki, more

Archiv der Pharmazie > 349 > 12 > 889 - 903

In the search for potential psychotropic agents, a new series of 3,7‐dimethyl‐ and 1,3‐dimethyl‐8‐alkoxypurine‐2,6‐dione derivatives of arylpiperazines, perhydroisoquinolines, or tetrahydroisoquinolines with flexible alkylene spacers (5–16 and 21–32) were synthesized and evaluated for 5‐HT_1A/5‐HT₇ receptor affinities as well as PDE4B1 and PDE10A inhibitory properties. The 1‐(4‐(4‐(2‐hydroxyphenyl)piperazin‐1‐yl)butyl)‐3,7‐dimethyl‐8‐propoxypurine‐2,6‐dione...

article

Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT6 receptor antagonists. Design, synthesis and biological evaluation

Anna Więckowska, Marcin Kołaczkowski, Adam Bucki, Justyna Godyń, more

European Journal of Medicinal Chemistry > 2016 > 124 > C > 63-81

As currently postulated, a complex treatment may be key to an effective therapy for Alzheimer's disease (AD). Recent clinical trials in patients with moderate AD have shown a superior effect of the combination therapy of donepezil (a selective acetylcholinesterase inhibitor) with idalopirdine (a 5-HT₆ receptor antagonist) over monotherapy with donepezil. Here, we present the first report on the design,...

article

Structure–5‐HT/D₂ Receptor Affinity Relationship in a New Group of 1‐Arylpiperazynylalkyl Derivatives of 8‐Dialkylamino‐3,7‐dimethyl‐1H‐purine‐2,6(3H,7H)‐dione

Paweł Żmudzki, Grzegorz Satała, Grażyna Chłoń‐Rzepa, Andrzej J. Bojarski, more

Archiv der Pharmazie > 349 > 10 > 774 - 784

In our previous papers, we have reported that some 8‐amino‐1,3‐dimethyl‐1H‐purine‐2,6(3H,7H)‐dione derivatives possessed high affinity and displayed agonistic, partial agonistic, or antagonistic activity for serotonin 5‐HT_1A and dopamine D₂ receptors. In order to examine further the influence of the substituent in the position 8 of the purine moiety and the influence of the xanthine core on the affinity...

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HBK-7 — A new xanthone derivative and a 5-HT1A receptor antagonist with antidepressant-like properties

Karolina Pytka, Grzegorz Kazek, Agata Siwek, Barbara Mordyl, more

Pharmacology Biochemistry and Behavior > 2016 > 146-147 > C > 35-43

Xanthone derivatives possess many biological properties, including neuroprotective, antioxidant or antidepressant-like. In this study we aimed to investigate antidepressant- and anxiolytic-like properties of a new xanthone derivative – 6-methoxy-4-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one (HBK-7), as well as its possible mechanism of action, and the influence on cognitive and motor function...

article

Pyrrolidin-2-one derivatives may reduce body weight in rats with diet-induced obesity

Magdalena Dudek, Joanna Knutelska, Marek Bednarski, Leszek Nowiński, more

European Journal of Pharmacology > 2016 > 776 > C > 146-155

Obesity affects an increasing number of individuals in the human population and significant importance is attached to research leading to the discovery of drug which would effectively reduce weight. The search for new drugs with anorectic activity and acting within the adrenergic system has attracted the interest of researchers. This study concerns the experimental effects on body weight of α₂-adrenoceptor...

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The antidepressant-like activity of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one involves serotonergic 5-HT1A and 5-HT2A/C receptors activation

Karolina Pytka, Maria Walczak, Agnieszka Kij, Anna Rapacz, more

European Journal of Pharmacology > 2015 > 764 > Complete > 537-546

Xanthone derivatives have been shown to posses many biological properties. Some of them act within the central nervous system and show neuroprotective or antidepressant-like properties. Taking this into account we investigated antidepressant-like activity in mice and the possible mechanism of action of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one (HBK-11) – a new xanthone derivative...

article

Novel spirohydantoin derivative as a potent multireceptor-active antipsychotic and antidepressant agent

Anna Czopek, Marcin Kołaczkowski, Adam Bucki, Hanna Byrtus, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 13 > 3436-3447

A series of novel spirohydantoin derivatives with arylpiperazinylbutyl moiety were synthesized and evaluated for serotonin 5-HT_1A, 5-HT_2A, 5-HT₇ and dopamine D₂ receptors. Based on these data, four compounds were selected for further binding affinity assays on dopamine D₁, D₃, D₄, and 5-HT_2C, 5-HT₆ as well as adrenergic α₁ and α_2C receptors, which are involved in various CNS diseases such as schizophrenia,...

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Structure–activity relationships and molecular studies of novel arylpiperazinylalkyl purine-2,4-diones and purine-2,4,8-triones with antidepressant and anxiolytic-like activity

Agnieszka Zagórska, Marcin Kołaczkowski, Adam Bucki, Agata Siwek, more

European Journal of Medicinal Chemistry > 2015 > 97 > Complete > 142-154

A novel series of arylpiperazinylalkyl purine-2,4-diones (4–27) and purine-2,4,8-triones (31–38) was synthesized and tested to evaluated their affinity for the serotoninergic (5-HT1A, 5-HT6, 5-HT7) and dopaminergic (D2) receptors. Compounds with purine-2,4-dione nucleus generally had affinity values higher than the corresponding purine-2,4,8-trione compounds. A spectrum of receptor activities was...

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Antinociceptive, anti-inflammatory and smooth muscle relaxant activities of the pyrrolo[3,4-d]pyridazinone derivatives: Possible mechanisms of action

Szczepan Mogilski, Monika Kubacka, Aleksandra Redzicka, Grzegorz Kazek, more

Pharmacology, Biochemistry and Behavior > 2015 > 133 > Complete > 99-110

The aim of this study was to evaluate the analgesic as well as anti-inflammatory activities of the new pyrrolo[3,4-d]pyridazinone derivatives. Moreover, the present study attempted to assess some of the mechanisms involved in the pharmacological activity of these compounds.In the previous studies it was shown that these compounds were highly active in the phenylbenzoquinone-induced ‘writhing syndrome’...

article

Structure–5‐HT Receptor Affinity Relationship in a New Group of 7‐Arylpiperazynylalkyl and 7‐Tetrahydroisoquinolinylalkyl Derivatives of 8‐Amino‐1,3‐dimethyl‐1H‐purine‐2,6(3H,7H)‐dione

Paweł Żmudzki, Grażyna Chłoń‐Rzepa, Andrzej J. Bojarski, Małgorzata Zygmunt, more

Archiv der Pharmazie > 348 > 4 > 229 - 241

In our previous paper, we have reported that some 8‐alkoxy‐1,3‐dimethyl‐1H‐purine‐2,6(3H,7H)‐dione derivatives possessed high affinity and displayed agonistic activity for the serotonin 5‐HT_1A receptor. In order to examine the influence of the substituent in the position 8 of the purine moiety on the affinity for the serotonin 5‐HT_1A, 5‐HT_2A, and 5‐HT₇ receptors, a series of 7‐arylpiperazynylalkyl...

article

Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia

Marcin Kołaczkowski, Monika Marcinkowska, Adam Bucki, Joanna Śniecikowska, more

European Journal of Medicinal Chemistry > 2015 > 92 > C > 221-235

We describe a novel class of designed multiple ligands (DMLs) combining serotonin 5-HT₆ receptor (5-HT₆R) antagonism with dopamine D₂ receptor (D₂R) partial agonism. Prototype hybrid molecules were designed using docking to receptor homology models. Diverse pharmacophore moieties yielded 3 series of hybrids with varying in vitro properties at 5-HT₆R and D₂R, and at M₁ receptor and hERG channel antitargets...

article

Synthesis and Pharmacological Evaluation of Novel Tricyclic[2,1‐f]theophylline Derivatives

Agnieszka Zagórska, Maciej Pawłowski, Agata Siwek, Grzegorz Kazek, more

Archiv der Pharmazie > 346 > 11 > 832 - 839

The multireceptor strategy was implemented to obtain potential antipsychotics and/or antidepressants in a series of long‐chain arylpiperazines bearing a tricyclic theophylline fragment. Their binding profile toward monoaminergic receptors (α₁, 5‐HT_1A, 5‐HT_2A, 5‐HT₆, 5‐HT₇, D₂, D₃) was determined as well. The selected compounds 7 and 9 were tested in functional in vivo models and showed, like atypical...

article

Novel vanadyl complexes of acetoacetanilide: Synthesis, characterization and inhibition of proteintyrosine phosphatase

Ryszard Gryboś, Patrycja Paciorek, Janusz T. Szklarzewicz, Dariusz Matoga, more

Polyhedron > 2013 > 49 > 1 > 100-104

Three novel vanadyl complexes, [VO(OH)(aa)(Haa)]·Haa (1), [VO(aa) ₂ (H ₂ O)] (2) and [VO(OH)(aa)(Haa)] (3), were synthesized in the reaction between vanadyl sulfate and acetoacetanilide (Haa), with a stoichiometry of 1:2, in water/ethanol solution. These complexes have been characterized by elemental analysis, ESR, IR, UV–Vis spectroscopy and cyclic voltammetry. Their composition depends...

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