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161 results on '"Czopek, Anna"'

1. The use of non-steroidal anti-inflammatory drugs (NSAIDs) in clinical practice for the treatment of periodontitis: a narrative review

Author

Zajac-Grabiec Anna, Kuznik Magdalena, Penno Marta, Czopek Anna, and Miszczyk Justyna

Subjects
periodontitis, narrative review, nsaid, Medicine
Abstract

After dental caries, the most common multifactorial oral disease is periodontal disease. Periodontitis can result in biofilm and host dysbiosis, ultimately causing inflammation and destruction of periodontal tissues. This narrative review aimed to summarise and discuss the mechanism of action, categories and use of non-steroidal anti-inflammatory drugs (NSAIDs) in clinical practice in the treatment of periodontitis because of their analgesic, anti-inflammatory and reducing effects on platelet aggregation and thus bleeding. Also, this review illustrates the importance of studies demonstrating synergism between specialty drugs and their derivatives as valuable active substances. The eleven clinical trials conducted in small groups of adult volunteers (14-50) treated with various NSAIDs, e.g. aspirin, ibuprofen, diclofenac, ketoprofen and tenoxicam are discussed. The results of clinical trials have shown that the use of NSAIDs together with surgical intervention in the treatment of periodontal diseases produces beneficial effects as an adjunctive treatment. It is worth noting that these studies were conducted on small cohorts of adult volunteers, with variations in the duration of treatment and doses of administered drugs. Further research on the impact of NSAIDs administration on periodontal disease may provide in-depth knowledge of patient groups with different demographics, including age, gender and comorbidities. Additional research is necessary to explore the use of NSAIDs in combination with periodontitis treatment for different patient groups.

Published
2024
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6. An insight into the structure of 5-spiro aromatic derivatives of imidazolidine-2,4-dione, a new group of very potent inhibitors of tumor multidrug resistance in T-lymphoma cells

Author

Żesławska, Ewa, Kucwaj-Brysz, Katarzyna, Kincses, Annamária, Spengler, Gabriella, Szymańska, Ewa, Czopek, Anna, Marć, Małgorzata Anna, Kaczor, Aneta, Nitek, Wojciech, Domínguez-Álvarez, Enrique, Latacz, Gniewomir, Kieć-Kononowicz, Katarzyna, and Handzlik, Jadwiga

Published
2021
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7. Inhibitors of SARS-CoV-2 Main Protease (Mpro) as Anti-Coronavirus Agents.

Author

Zagórska, Agnieszka, Czopek, Anna, Fryc, Monika, and Jończyk, Jakub

Subjects
*PROTEIN-ligand interactions, *COVID-19 treatment, *PROTEIN structure, *ANTIVIRAL agents, *SARS-CoV-2
Abstract

The main protease (Mpro) of SARS-CoV-2 is an essential enzyme that plays a critical part in the virus's life cycle, making it a significant target for developing antiviral drugs. The inhibition of SARS-CoV-2 Mpro has emerged as a promising approach for developing therapeutic agents to treat COVID-19. This review explores the structure of the Mpro protein and analyzes the progress made in understanding protein–ligand interactions of Mpro inhibitors. It focuses on binding kinetics, origin, and the chemical structure of these inhibitors. The review provides an in-depth analysis of recent clinical trials involving covalent and non-covalent inhibitors and emerging dual inhibitors targeting SARS-CoV-2 Mpro. By integrating findings from the literature and ongoing clinical trials, this review captures the current state of research into Mpro inhibitors, offering a comprehensive understanding of challenges and directions in their future development as anti-coronavirus agents. This information provides new insights and inspiration for medicinal chemists, paving the way for developing more effective Mpro inhibitors as novel COVID-19 therapies. [ABSTRACT FROM AUTHOR]

Published
2024
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9. Drug Discovery and Development Targeting Dementia

Author

Zagórska, Agnieszka, Czopek, Anna, Fryc, Monika, Jaromin, Anna, Boyd, Ben J., Zagórska, Agnieszka, Czopek, Anna, Fryc, Monika, Jaromin, Anna, and Boyd, Ben J.

Abstract

Dementia, most often associated with neurodegenerative diseases, affects millions of people worldwide, predominantly the elderly. Unfortunately, no treatment is still available. Therefore, there is an urgent need to address this situation. This review presents the state of the art of drug discovery and developments in targeting dementia. Several approaches are discussed, such as drug repurposing, the use of small molecules, and phosphodiesterase inhibitors. Furthermore, the review also provides insights into clinical trials of these molecules. Emphasis has been placed on small molecules and multi-target-directed ligands, as well as disease-modifying therapies. Finally, attention is drawn to the possibilities of applications of nanotechnology in managing dementia.

Published
2023

17. The Development of the Innovative Synthesis Methodology of Albumin Nanoparticles Supported by Their Physicochemical, Cytotoxic and Hemolytic Evaluation

Author

Kudłacik-Kramarczyk, Sonia, primary, Drabczyk, Anna, additional, Głąb, Magdalena, additional, Gajda, Paweł, additional, Czopek, Anna, additional, Zagórska, Agnieszka, additional, Jaromin, Anna, additional, Gubernator, Jerzy, additional, Makara, Agnieszka, additional, and Tyliszczak, Bożena, additional

Published
2021
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28. Impact of N-Alkylamino Substituents on Serotonin Receptor (5-HTR) Affinity and Phosphodiesterase 10A (PDE10A) Inhibition of Isoindole-1,3-dione Derivatives

Author

Czopek, Anna, primary, Partyka, Anna, additional, Bucki, Adam, additional, Pawłowski, Maciej, additional, Kołaczkowski, Marcin, additional, Siwek, Agata, additional, Głuch-Lutwin, Monika, additional, Koczurkiewicz, Paulina, additional, Pękala, Elżbieta, additional, Jaromin, Anna, additional, Tyliszczak, Bożena, additional, Wesołowska, Anna, additional, and Zagórska, Agnieszka, additional

Published
2020
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30. Characteristics of metabolic stability and the cell permeability of 2-pyrimidynyl-piperazinyl-alkyl derivatives of 1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione with antidepressant- and anxiolytic-like activity

Author

Zagórska, Agnieszka, Partyka, Anna, Bucki, Adam, Kołaczkowski, Marcin, Jastrzębska-Więsek, Magdalena, Czopek, Anna, Siwek, Agata, Głuch-Lutwin, Monika, Bednarski, Marek, Bajda, Marek, Jończyk, Jakub, Piska, Kamil Tomasz, Koczurkiewicz, Paulina, Wesołowska, Anna, and Pawłowski, Maciej

Published
2019

32. Novel serotonin 5-HT2Areceptor antagonists derived from 4-phenylcyclohexane-5-spiro-and 5-methyl-5-phenyl-hydantoin, for use as potential antiplatelet agents

Author

Czopek, Anna, Kubacka, Monika, Bucki, Adam, Siwek, Agata, Filipek, Barbara, Pawłowski, Maciej, and Kołaczkowski, Marcin

Abstract

Background: Antiplatelet drugs have been used in the treatment of acute coronary syndromes and for the prevention of recurrent events. Unfortunately, many patients remain resistant to the available antiplatelet treatment. Therefore, there is a clinical need to synthesize novel antiplatelet agents, which would be associated with different pathways of platelet aggregation, to develop an alternative or additional treatment for resistant patients. Recent studies have revealed that 5-HT2Areceptor antagonists could constitute alternative antiplatelet therapy. Methods: Based on the structures of the conventional 5-HT2Areceptor ligands, two series of compounds with 4-phenylcyclohexane-5-spiro- or 5-methyl-5-phenyl-hydantoin core linked to various arylpiperazine moieties were synthesized and their affinity for 5-HT2Areceptor was assessed. Further, we evaluated their antagonistic potency at 5-HT2Areceptors using isolated rat aorta and cells expressing human 5-HT2Areceptors. Finally, we studied their anti-aggregation effect and compared it with ketanserin and sarpogrelate, the reference 5-HT2Areceptor antagonists. Moreover, the structure–activity relationships were studied following molecular docking to the 5-HT2Areceptor model. Results: Functional bioassays revealed some of the synthesized compounds to be moderate antagonists of 5-HT2Areceptors. Among them, 13, 8-phenyl-3-(3-(4-phenylpiperazin-1-yl)propyl)-1,3-diazaspiro[4.5]decane-2,4-dione, inhibited collagen stimulated aggregation (IC50= 27.3 μM) being more active than sarpogrelate (IC50= 66.8 μM) and comparable with ketanserin (IC50= 32.1 μM). Moreover, compounds 2–5, 9–11, 13, 14 inhibited 5-HT amplified, ADP- or collagen-induced aggregation. Conclusions: Our study confirmed that the 5-HT2Aantagonists effectively suppress platelet aggregation and remain an interesting option for the development of novel antiplatelet agents with an alternative mechanism of action.

Published
2021
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33. Evaluation of antiarrythmic activity of novel imidazo[2,1-F]purine-2,4-dione and imidazolidine-2,4-dione derivatives with aminoalkyl moieties

Author

Sapa, Jacek, Zygmunt, Malgorzata, Bednarski, Marek, Agata Siwek, Pawlowski, Maciej, Chlon-Rzepa, Grazyna, Czopek, Anna, and Zagorska, Agnieszka

Subjects
5-HT1A-receptors, antiarrhythmic, imidazo[2,1-f]purine-2,4-dione, α1-adrenoreceptors, imidazolidine-2,4-dione
Abstract

The main goal of this study was to assess antiarrhythmic activity of novel aminoalkyl derivatives of imidazo[2,1-f]purine-2,4-dione and imidazolidine-2,4-dione exerting α1 and 5-HT1A receptors affinity. Tested compounds produced prophylactic and therapeutic antiarrhythmic activity in an adrenaline-induced model of arrhythmia. The strongest antiarrhythmic activity as well as the highest α1-adrenoreceptor affinity (Ki = 13.9 nM) was found for 5-methyl-5-phenyl-3-[3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl]-imidazolidine-2,4- dione (12). The results indicated a correlation between α1-adrenoreceptor affinities and antiarrhythmic activity.

Published
2017

36. Characteristics of metabolic stability and the cell permeability of 2‐pyrimidinyl‐piperazinyl‐alkyl derivatives of 1H‐imidazo[2,1 ‐f ]purine‐2,4(3 H ,8 H )‐dione with antidepressant‐ and anxiolytic‐like activities

Author

Zagórska, Agnieszka, primary, Partyka, Anna, additional, Bucki, Adam, additional, Kołaczkowski, Marcin, additional, Jastrzębska‐Więsek, Magdalena, additional, Czopek, Anna, additional, Siwek, Agata, additional, Głuch‐Lutwin, Monika, additional, Bednarski, Marek, additional, Bajda, Marek, additional, Jończyk, Jakub, additional, Piska, Kamil, additional, Koczurkiewicz, Paulina, additional, Wesołowska, Anna, additional, and Pawłowski, Maciej, additional

Published
2018
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41. Reversed-phase high performance liquid chromatography study of lipophilicity of imidazo[2,1-f]theophylline derivatives

Author

Zagórska, Agnieszka, Czopek, Anna, Pełka, Karolina, Bajda, Marek, Stanisz-Wallis, Krystyna, and Pawłowski, Maciej

Subjects
logP, tricyclic theophylline derivatives, lipophilicity
Abstract

The present study is a part of our physicochemical and pharmacological studies in a group of tricyclic theophylline derivatives. The investigated compounds exhibit different pharmacological profiles in comparison to theophylline and have been tested as potential antidepressant and/or antipsychotic agents. The differences in pharmacological action between theophylline and their tricyclic derivatives can be explained by their various physicochemical properties, especially lipophilicity. The chromatographic behavior of twenty three derivatives of imidazo[2,1-f]theophylline was investigated, using reversed-phase high performance liquid chromatography (RP-HPLC) method. Moreover, partition coefficients and selected pharmacokinetic parameters were calculated computationally. Principal component analysis (PCA) method was used to establish the relationship between obtained experimental and computational parameters.

Published
2015

42. Reversed-phase TLC study of some long chain arylpiperazine of imidazolidine-2,4-dione and imidazo[2,1-φ]purine-2,4-dione derivatives

Author

Zagórska, Agnieszka, Czopek, Anna, Pełka, Karolina, Stanisz-Wallis, Krystyna, and Pawłowski, Maciej

Subjects
lipophilicity, imidazo[2,1-f]purine-2,4-diones, imidazolidine-2,4-diones
Abstract

The chromatographic parameters of arylpiperazinylpropyl derivatives of imidazolidine-2,4-dione and imidazo[2,1-f]purine-2,4-dione were investigated using reversed-phase thin layer chromatography method. The results revealed that RM0 of investigated compounds depended on substituent in arylpiperazinyl fragment as well as on a nature of (cycloalkyl)aromatic ring at 5 position of imidazolidine-2,4-dione and at 7 position of imidazo[2,1-f]theophylline. The RM0 parameters were compared with computationally calculated partition coefficients values by principal component analysis (PCA). To verify the influence of lipophilic parameter of investigated compounds on their biological activity the statistical analysis of Mann-Whitney was performed.

Published
2014

43. Zastosowanie leków biologicznych w terapii łuszczycy.

Author

Partyka, Anna, Czopek, Anna, Stanisz-Wallis, Krystyna, and Zagórska, Agnieszka

Abstract

Dermatoses are the group of diseases which involve all layers of the skin from the epidermis through the dermis and subcutaneous tissue, till appendages. The global burden of skin disease in populations is not currently monitored, therefore there is no data on the prevalence of skin diseases in the general population. However, from the epidemiological point of view, it is possible to point out the most common dermatoses and among them distinguish these diseases, which belong to chronic conditions with immunological origin e.g. atopic dermatitis, psoriasis, pemphigus, vitiligo and alopecia areata. Due to conducted studies and better diagnostics, unknown pathomechanisms of dermatoses are discovered and consequently new treatment methods are implemented. The therapeutic progress in the symptomatic treatment of autoimmune skin diseases is related to the introduction on the market of biological medical products called biopharmaceuticals. In this manuscript, the characterization of biopharmaceuticals is presented in terms of their applicability in the treatment of psoriasis. Psoriasis is the chronic dermatological disease with inflammatory response and non-infective character, which shows significant variations in the prevalence of European population. Typical symptoms of psoriasis are red, raised skin areas, covered with silvery scales, mainly appears within the upper and lower extremities face and head. Further in the manuscript, psoriasis is discussed as a public health problem, the pathogenesis of this disease is described and the characterization of the biopharmaceuticals used in psoriasis is presented. In the last part, the results of a systematic literature review (meta-analysis) on the etanercept, the biopharmaceutical used in psoriasis, is discussed. [ABSTRACT FROM AUTHOR]

Published
2018
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50. Synthesis and pharmacological evaluation of new 5-(cyclo)alkyl-5-phenyl- and 5-spiroimidazolidine-2,4-dione derivatives. Novel 5-HT1A receptor agonist with potential antidepressant and anxiolytic activity

Author

Czopek, Anna, primary, Byrtus, Hanna, additional, Kołaczkowski, Marcin, additional, Pawłowski, Maciej, additional, Dybała, Małgorzata, additional, Nowak, Gabriel, additional, Tatarczyńska, Ewa, additional, Wesołowska, Anna, additional, and Chojnacka-Wójcik, Ewa, additional

Published
2010
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