LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 10 of total 34

Search options

  1. Article: Drug Discovery and Development Targeting Dementia.

    Zagórska, Agnieszka / Czopek, Anna / Fryc, Monika / Jaromin, Anna / Boyd, Ben J

    Pharmaceuticals (Basel, Switzerland)

    2023  Volume 16, Issue 2

    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 ... ...

    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.
    Language English
    Publishing date 2023-01-19
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2193542-7
    ISSN 1424-8247
    ISSN 1424-8247
    DOI 10.3390/ph16020151
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  2. Article ; Online: Antinociceptive and Antiallodynic Activity of Some 3-(3-Methylthiophen-2-yl)pyrrolidine-2,5-dione Derivatives in Mouse Models of Tonic and Neuropathic Pain.

    Dziubina, Anna / Rapacz, Anna / Czopek, Anna / Góra, Małgorzata / Obniska, Jolanta / Kamiński, Krzysztof

    International journal of molecular sciences

    2022  Volume 23, Issue 7

    Abstract: Antiseizure drugs (ASDs) are commonly used to treat a wide range of nonepileptic conditions, including pain. In this context, the analgesic effect of four pyrrolidine-2,5-dione derivatives ( ... ...

    Abstract Antiseizure drugs (ASDs) are commonly used to treat a wide range of nonepileptic conditions, including pain. In this context, the analgesic effect of four pyrrolidine-2,5-dione derivatives (compounds
    MeSH term(s) Analgesics/pharmacology ; Analgesics/therapeutic use ; Animals ; Diabetic Neuropathies/drug therapy ; Disease Models, Animal ; Hyperalgesia/drug therapy ; Mice ; Neuralgia/drug therapy ; Oxaliplatin/therapeutic use ; Pyrrolidines ; Streptozocin
    Chemical Substances Analgesics ; Pyrrolidines ; pyrrolidine-2,5-dione ; Oxaliplatin (04ZR38536J) ; Streptozocin (5W494URQ81)
    Language English
    Publishing date 2022-04-06
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2019364-6
    ISSN 1422-0067 ; 1422-0067 ; 1661-6596
    ISSN (online) 1422-0067
    ISSN 1422-0067 ; 1661-6596
    DOI 10.3390/ijms23074057
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  3. Article: Novel serotonin 5-HT

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

    Pharmacological reports : PR

    2021  Volume 73, Issue 5, Page(s) 1361–1372

    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 ... ...

    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-HT
    Methods: Based on the structures of the conventional 5-HT
    Results: Functional bioassays revealed some of the synthesized compounds to be moderate antagonists of 5-HT
    Conclusions: Our study confirmed that the 5-HT
    MeSH term(s) Animals ; Aorta ; CHO Cells ; Cricetinae ; Cricetulus ; Humans ; Hydantoins/chemical synthesis ; Hydantoins/pharmacology ; Mianserin/pharmacology ; Models, Molecular ; Molecular Structure ; Platelet Aggregation Inhibitors/chemical synthesis ; Platelet Aggregation Inhibitors/pharmacology ; Protein Conformation ; Rats ; Serotonin 5-HT2 Receptor Antagonists/chemical synthesis ; Serotonin 5-HT2 Receptor Antagonists/pharmacology
    Chemical Substances Hydantoins ; Platelet Aggregation Inhibitors ; Serotonin 5-HT2 Receptor Antagonists ; Mianserin (250PJI13LM)
    Language English
    Publishing date 2021-06-11
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2186248-5
    ISSN 1734-1140
    ISSN 1734-1140
    DOI 10.1007/s43440-021-00284-6
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  4. Article ; Online: Synthesis and Antiplasmodial Activity of Novel Bioinspired Imidazolidinedione Derivatives.

    Jaromin, Anna / Czopek, Anna / Parapini, Silvia / Basilico, Nicoletta / Misiak, Ernest / Gubernator, Jerzy / Zagórska, Agnieszka

    Biomolecules

    2020  Volume 11, Issue 1

    Abstract: Malaria is an enormous threat to public health, due to the emergence ... ...

    Abstract Malaria is an enormous threat to public health, due to the emergence of
    MeSH term(s) Antimalarials/chemical synthesis ; Antimalarials/chemistry ; Antimalarials/pharmacology ; Cell Line ; Chemistry Techniques, Synthetic ; Chloroquine/pharmacology ; Drug Discovery ; Drug Resistance ; Hemolysis/drug effects ; Humans ; Imidazolidines/chemical synthesis ; Imidazolidines/chemistry ; Imidazolidines/pharmacology ; Malaria, Falciparum/drug therapy ; Plasmodium falciparum/drug effects
    Chemical Substances Antimalarials ; Imidazolidines ; imidazolidine-2,4-dione ; Chloroquine (886U3H6UFF)
    Language English
    Publishing date 2020-12-29
    Publishing country Switzerland
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2701262-1
    ISSN 2218-273X ; 2218-273X
    ISSN (online) 2218-273X
    ISSN 2218-273X
    DOI 10.3390/biom11010033
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  5. Article ; Online: Synthesis, computational simulations and biological evaluation of new dual 5HT

    Zagórska, Agnieszka / Partyka, Anna / Jastrzębska-Więsek, Magdalena / Czopek, Anna / Fryc, Monika / Siwek, Agata / Głuch-Lutwin, Monika / Mordyl, Barbara / Maślanka, Anna / Jaromin, Anna / Kurczab, Rafał

    Bioorganic chemistry

    2023  Volume 139, Page(s) 106737

    Abstract: The new dual ... ...

    Abstract The new dual 5HT
    MeSH term(s) Animals ; Ligands ; Molecular Docking Simulation ; Fluorine ; Antidepressive Agents/pharmacology ; Structure-Activity Relationship ; Purines/chemistry
    Chemical Substances Ligands ; Fluorine (284SYP0193) ; Antidepressive Agents ; Purines
    Language English
    Publishing date 2023-07-19
    Publishing country United States
    Document type Journal Article
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2023.106737
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  6. Article: Design, Synthesis, and In Vitro Antiproliferative Activity of Hydantoin and Purine Derivatives with the 4-Acetylphenylpiperazinylalkyl Moiety.

    Zagórska, Agnieszka / Czopek, Anna / Jaromin, Anna / Mielczarek-Puta, Magdalena / Struga, Marta / Stary, Dorota / Bajda, Marek

    Materials (Basel, Switzerland)

    2021  Volume 14, Issue 15

    Abstract: Cancer represents one of the most serious health problems and the second leading cause of death around the world. Heterocycles, due to their prevalence in nature as well as their structural and chemical diversity, play an immensely important role in anti- ...

    Abstract Cancer represents one of the most serious health problems and the second leading cause of death around the world. Heterocycles, due to their prevalence in nature as well as their structural and chemical diversity, play an immensely important role in anti-cancer drug discovery. In this paper, a series of hydantoin and purine derivatives containing a 4-acetylphenylpiperazinylalkyl moiety were designed, synthesized, and biologically evaluated for their anticancer activity on selected cancer cell lines (PC3, SW480, SW620). Compound
    Language English
    Publishing date 2021-07-26
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2487261-1
    ISSN 1996-1944
    ISSN 1996-1944
    DOI 10.3390/ma14154156
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  7. Article: Synthesis and Physicochemical Evaluation of Bees' Chitosan-Based Hydrogels Modified with Yellow Tea Extract.

    Kudłacik-Kramarczyk, Sonia / Drabczyk, Anna / Głąb, Magdalena / Gajda, Paweł / Jaromin, Anna / Czopek, Anna / Zagórska, Agnieszka / Tyliszczak, Bożena

    Materials (Basel, Switzerland)

    2021  Volume 14, Issue 12

    Abstract: The novelty of the research involves designing the measurement methodology aimed at determining the structure-property relationships in the chitosan-based hydrogels containing yellow tea extract. Performed investigations allowed us to determine the ... ...

    Abstract The novelty of the research involves designing the measurement methodology aimed at determining the structure-property relationships in the chitosan-based hydrogels containing yellow tea extract. Performed investigations allowed us to determine the swelling properties of hydrogels in selected time intervals, evaluate the mutual interactions between the hydrogels and simulated physiological liquids via pH measurements and directly assess the impact of such interactions on the chemical structure of hydrogels using Fourier transform infrared (FT-IR) spectroscopy and their wettability by the measurements of the flatness of the drop on the surface of the tested samples via the static drop method. Next, the surface morphology of hydrogels was characterized by the Scanning Electron Miscorcopy (SEM) and their elasticity under the tension applied was also verified. It was proved that incubation in simulated physiological liquids resulted in a decrease in contact angles of hydrogels, even by 60%. This also caused their certain degradation which was reflected in lower intensities of bands on FT-IR spectra. Further, 23%
    Language English
    Publishing date 2021-06-18
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2487261-1
    ISSN 1996-1944
    ISSN 1996-1944
    DOI 10.3390/ma14123379
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  8. Article ; Online: Synthesis, Anticonvulsant, and Antinociceptive Activity of New 3-(2-Chlorophenyl)- and 3-(3-Chlorophenyl)-2,5-dioxo-pyrrolidin-1-yl-acetamides.

    Góra, Małgorzata / Czopek, Anna / Rapacz, Anna / Gębska, Anna / Wójcik-Pszczoła, Katarzyna / Pękala, Elżbieta / Kamiński, Krzysztof

    Molecules (Basel, Switzerland)

    2021  Volume 26, Issue 6

    Abstract: The new series of 3-(2-chlorophenyl)- and 3-(3-chlorophenyl)-pyrrolidine-2,5-dione-acetamide derivatives as potential anticonvulsant and analgesic agents was synthesized. The compounds obtained were evaluated in the following acute models of epilepsy: ... ...

    Abstract The new series of 3-(2-chlorophenyl)- and 3-(3-chlorophenyl)-pyrrolidine-2,5-dione-acetamide derivatives as potential anticonvulsant and analgesic agents was synthesized. The compounds obtained were evaluated in the following acute models of epilepsy: maximal electroshock (MES), psychomotor (6 Hz, 32 mA), and subcutaneous pentylenetetrazole (
    MeSH term(s) Analgesics/chemical synthesis ; Analgesics/chemistry ; Analgesics/pharmacology ; Animals ; Anticonvulsants/chemical synthesis ; Anticonvulsants/chemistry ; Anticonvulsants/pharmacology ; Cell Line ; Disease Models, Animal ; Drug Evaluation, Preclinical ; Hep G2 Cells ; Humans ; In Vitro Techniques ; Male ; Mice ; Molecular Structure ; Neuralgia/drug therapy ; Pyrrolidines/chemical synthesis ; Pyrrolidines/chemistry ; Pyrrolidines/pharmacology ; Seizures/drug therapy ; Structure-Activity Relationship
    Chemical Substances Analgesics ; Anticonvulsants ; Pyrrolidines
    Language English
    Publishing date 2021-03-12
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules26061564
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  9. Article ; Online: Design, Synthesis and Biological Activity of New Amides Derived from 3-Benzhydryl and 3-sec-Butyl-2,5-dioxo-pyrrolidin-1-yl-acetic Acid.

    Góra, Małgorzata / Czopek, Anna / Rapacz, Anna / Giza, Agnieszka / Koczurkiewicz-Adamczyk, Paulina / Pękala, Elżbieta / Obniska, Jolanta / Kamiński, Krzysztof

    ChemMedChem

    2021  Volume 16, Issue 10, Page(s) 1619–1630

    Abstract: The aim of this study was to design and synthesize two new series of pyrrolidine-2,5-dione-acetamides with a benzhydryl or sec-butyl group at position 3 as potential anticonvulsants. Their anticonvulsant activity was evaluated in standard animal models ... ...

    Abstract The aim of this study was to design and synthesize two new series of pyrrolidine-2,5-dione-acetamides with a benzhydryl or sec-butyl group at position 3 as potential anticonvulsants. Their anticonvulsant activity was evaluated in standard animal models of epilepsy: the maximal electroshock (MES), the 6 Hz, and the subcutaneous pentylenetetrazole (scPTZ) tests. The in vivo studies revealed the most potent anticonvulsant activity for 15 (3-(sec-butyl)-1-(2-(4-(3-trifluoromethylphenyl)piperazin-1-yl)-2-oxoethyl)pyrrolidine-2,5-dione), with ED
    MeSH term(s) Acetic Acid/chemical synthesis ; Acetic Acid/chemistry ; Acetic Acid/pharmacology ; Amides/chemical synthesis ; Amides/chemistry ; Amides/pharmacology ; Analgesics/chemical synthesis ; Analgesics/chemistry ; Analgesics/pharmacology ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Design ; Drug Screening Assays, Antitumor ; Formaldehyde ; Hep G2 Cells ; Humans ; Molecular Structure ; Pain/chemically induced ; Pain/drug therapy ; Seizures/chemically induced ; Seizures/drug therapy ; Structure-Activity Relationship
    Chemical Substances Amides ; Analgesics ; Antineoplastic Agents ; Formaldehyde (1HG84L3525) ; Acetic Acid (Q40Q9N063P)
    Language English
    Publishing date 2021-03-02
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2218496-X
    ISSN 1860-7187 ; 1860-7179
    ISSN (online) 1860-7187
    ISSN 1860-7179
    DOI 10.1002/cmdc.202001007
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

  10. Article ; Online: Synthesis, Anticonvulsant and Antinociceptive Activity of New Hybrid Compounds: Derivatives of 3-(3-Methylthiophen-2-yl)-pyrrolidine-2,5-dione.

    Góra, Małgorzata / Czopek, Anna / Rapacz, Anna / Dziubina, Anna / Głuch-Lutwin, Monika / Mordyl, Barbara / Obniska, Jolanta

    International journal of molecular sciences

    2020  Volume 21, Issue 16

    Abstract: The present study aimed to design and synthesize a new series of hybrid compounds with pyrrolidine-2,5-dione and thiophene rings in the structure as potential anticonvulsant and antinociceptive agents. For this purpose, we obtained a series of new ... ...

    Abstract The present study aimed to design and synthesize a new series of hybrid compounds with pyrrolidine-2,5-dione and thiophene rings in the structure as potential anticonvulsant and antinociceptive agents. For this purpose, we obtained a series of new compounds and evaluated their anticonvulsant activity in animal models of epilepsy (maximal electroshock (MES), psychomotor (6 Hz), and subcutaneous pentylenetetrazole (
    MeSH term(s) Analgesics/chemical synthesis ; Analgesics/chemistry ; Analgesics/pharmacology ; Animals ; Anticonvulsants/chemical synthesis ; Anticonvulsants/chemistry ; Anticonvulsants/pharmacology ; Cell Survival/drug effects ; Hep G2 Cells ; Humans ; Male ; Mice ; Pyrrolidines/chemical synthesis ; Pyrrolidines/chemistry ; Pyrrolidines/pharmacology
    Chemical Substances Analgesics ; Anticonvulsants ; Pyrrolidines ; pyrrolidine-2,5-dione
    Keywords covid19
    Language English
    Publishing date 2020-08-11
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2019364-6
    ISSN 1422-0067 ; 1422-0067 ; 1661-6596
    ISSN (online) 1422-0067
    ISSN 1422-0067 ; 1661-6596
    DOI 10.3390/ijms21165750
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

To top