LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 10 of total 50

Search options

  1. Article ; Online: Phosphodiesterase 10 (PDE10) inhibitors: an updated patent review (2014-present).

    Zagórska, Agnieszka

    Expert opinion on therapeutic patents

    2019  Volume 30, Issue 2, Page(s) 147–157

    Abstract: ... ...

    Abstract Introduction
    MeSH term(s) Animals ; Cyclic AMP/metabolism ; Cyclic GMP/metabolism ; Drug Development ; Drug Discovery/methods ; Humans ; Patents as Topic ; Phosphodiesterase Inhibitors/administration & dosage ; Phosphodiesterase Inhibitors/pharmacology ; Phosphoric Diester Hydrolases/drug effects ; Phosphoric Diester Hydrolases/metabolism ; Schizophrenia/drug therapy
    Chemical Substances Phosphodiesterase Inhibitors ; Cyclic AMP (E0399OZS9N) ; PDE10A protein, human (EC 3.1.4.-) ; Phosphoric Diester Hydrolases (EC 3.1.4.-) ; Cyclic GMP (H2D2X058MU)
    Language English
    Publishing date 2019-12-30
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 1186201-4
    ISSN 1744-7674 ; 0962-2594 ; 1354-3776
    ISSN (online) 1744-7674
    ISSN 0962-2594 ; 1354-3776
    DOI 10.1080/13543776.2020.1709444
    Database MEDical Literature Analysis and Retrieval System OnLINE

    Full text online

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 3962: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  2. Article ; Online: Antimalarials Targeting the Malaria Parasite Cation ATPase

    Zagórska, Agnieszka / Jaromin, Anna

    Current topics in medicinal chemistry

    2022  Volume 23, Issue 3, Page(s) 214–226

    Abstract: Malaria, caused by parasites of the Plasmodium species and transmitted through the bites of infected female Anopheles mosquitoes, is still a fatal and dangerous disease in mainly tropical and subtropical regions. The widespread resistance of P. ... ...

    Abstract Malaria, caused by parasites of the Plasmodium species and transmitted through the bites of infected female Anopheles mosquitoes, is still a fatal and dangerous disease in mainly tropical and subtropical regions. The widespread resistance of P. falciparum to antimalarial drugs forces the search for new molecules with activity against this parasite. While a large number of compounds can inhibit P. falciparum growth in vitro, unfortunately, only a limited number of targets have been identified so far. One of the most promising approaches has been the identification of effective inhibitors of P-type cation-transporter ATPase 4 (PfATP4) in P. falciparum. PfATP4 is a Na+ efflux pump that maintains a low cytosolic Na+ in the parasite. Thus, upon treatment with PfATP4 inhibitors, the parasites rapidly accumulate Na+, which triggers processes leading to parasite death. PfATP4 is present in the parasite plasma membrane but is absent in mammals; its exclusivity thus makes it a good antimalarial drug target. The current review presents PfATP4 function in the context of the pharmacological influence of its inhibitors. In addition, compounds with inhibitory activities belonging to spiroindolones, dihydroisoquinolones, aminopyrazoles, pyrazoleamides, and 4-cyano-3-methylisoquinolines, are also reviewed. Particular emphasis is placed on the results of preclinical and clinical studies in which their effectiveness was tested. PfATP4-associated antimalarials rapidly cleared parasites in mouse models and preliminary human trials. These findings highlight a fundamental biochemical mechanism sensitive to pharmacological intervention that can form a medicinal chemistry approach for antimalarial drug design to create new molecules with potent PfATP4 inhibitory activity.
    MeSH term(s) Animals ; Mice ; Female ; Humans ; Adenosine Triphosphatases/metabolism ; Antimalarials/chemistry ; Parasites ; Plasmodium falciparum ; Malaria/drug therapy ; Cations/metabolism ; Cations/pharmacology ; Cations/therapeutic use ; Malaria, Falciparum/drug therapy ; Malaria, Falciparum/parasitology ; Mammals/metabolism
    Chemical Substances Adenosine Triphosphatases (EC 3.6.1.-) ; Antimalarials ; Cations
    Language English
    Publishing date 2022-12-01
    Publishing country United Arab Emirates
    Document type Review ; Journal Article
    ZDB-ID 2064823-6
    ISSN 1873-4294 ; 1568-0266
    ISSN (online) 1873-4294
    ISSN 1568-0266
    DOI 10.2174/1568026623666221121154354
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 5572: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  3. Article ; Online: Perspectives for New and More Efficient Multifunctional Ligands for Alzheimer's Disease Therapy.

    Zagórska, Agnieszka / Jaromin, Anna

    Molecules (Basel, Switzerland)

    2020  Volume 25, Issue 15

    Abstract: Despite tremendous research efforts at every level, globally, there is still a lack of effective drugs for the treatment of Alzheimer's disease (AD). The biochemical mechanisms of this devastating neurodegenerative disease are not yet clearly understood. ...

    Abstract Despite tremendous research efforts at every level, globally, there is still a lack of effective drugs for the treatment of Alzheimer's disease (AD). The biochemical mechanisms of this devastating neurodegenerative disease are not yet clearly understood. This review analyses the relevance of multiple ligands in drug discovery for AD as a versatile toolbox for a polypharmacological approach to AD. Herein, we highlight major targets associated with AD, ranging from acetylcholine esterase (AChE), beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1), glycogen synthase kinase 3 beta (GSK-3β),
    MeSH term(s) Acetylcholinesterase ; Alzheimer Disease/drug therapy ; Alzheimer Disease/metabolism ; Amyloid Precursor Protein Secretases/antagonists & inhibitors ; Aspartic Acid Endopeptidases/antagonists & inhibitors ; Clinical Trials as Topic ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; GPI-Linked Proteins/antagonists & inhibitors ; Glycogen Synthase Kinase 3 beta/antagonists & inhibitors ; Humans ; Ligands ; Molecular Structure ; Monoamine Oxidase/metabolism ; Phosphoric Diester Hydrolases/metabolism ; Polypharmacology ; Receptors, Histamine H3/metabolism ; Receptors, N-Methyl-D-Aspartate/antagonists & inhibitors ; Receptors, Serotonin/metabolism
    Chemical Substances Enzyme Inhibitors ; GPI-Linked Proteins ; Ligands ; Receptors, Histamine H3 ; Receptors, N-Methyl-D-Aspartate ; Receptors, Serotonin ; Monoamine Oxidase (EC 1.4.3.4) ; GSK3B protein, human (EC 2.7.11.1) ; Glycogen Synthase Kinase 3 beta (EC 2.7.11.1) ; ACHE protein, human (EC 3.1.1.7) ; Acetylcholinesterase (EC 3.1.1.7) ; Phosphoric Diester Hydrolases (EC 3.1.4.-) ; Amyloid Precursor Protein Secretases (EC 3.4.-) ; Aspartic Acid Endopeptidases (EC 3.4.23.-) ; BACE1 protein, human (EC 3.4.23.46)
    Language English
    Publishing date 2020-07-23
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules25153337
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.MO 81: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  4. 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

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  5. Article: Efficient One-Pot Synthesis of Novel Caffeic Acid Derivatives as Potential Antimalarials.

    Sidoryk, Katarzyna / Parapini, Silvia / Basilico, Nicoletta / Zaremba-Czogalla, Magdalena / Kubiszewski, Marek / Cybulski, Marcin / Gubernator, Jerzy / Zagórska, Agnieszka / Jaromin, Anna

    Journal of parasitology research

    2023  Volume 2023, Page(s) 6675081

    Abstract: New protocol for the preparation of the novel caffeic acid derivatives using the Wittig reaction has been applied to follow the principles of green chemistry. The compounds have been evaluated against chloroquine-sensitive and chloroquine- ... ...

    Abstract New protocol for the preparation of the novel caffeic acid derivatives using the Wittig reaction has been applied to follow the principles of green chemistry. The compounds have been evaluated against chloroquine-sensitive and chloroquine-resistant
    Language English
    Publishing date 2023-11-24
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2563542-6
    ISSN 2090-0031 ; 2090-0023
    ISSN (online) 2090-0031
    ISSN 2090-0023
    DOI 10.1155/2023/6675081
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  6. Article ; Online: Exploring the antiplatelet activity of serotonin 5-HT

    Marcinkowska, Monika / Kubacka, Monika / Zagorska, Agnieszka / Jaromin, Anna / Fajkis-Zajaczkowska, Nikola / Kolaczkowski, Marcin

    Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

    2021  Volume 145, Page(s) 112424

    Abstract: Small drug-like molecules that can block the function of serotonin 5- ... ...

    Abstract Small drug-like molecules that can block the function of serotonin 5-HT
    MeSH term(s) Animals ; Cardiovascular Diseases/prevention & control ; Humans ; Isoxazoles/chemistry ; Isoxazoles/pharmacology ; Isoxazoles/toxicity ; Male ; Platelet Aggregation/drug effects ; Platelet Aggregation Inhibitors/chemistry ; Platelet Aggregation Inhibitors/pharmacology ; Platelet Aggregation Inhibitors/toxicity ; Rats ; Rats, Wistar ; Serotonin 5-HT2 Receptor Antagonists/chemistry ; Serotonin 5-HT2 Receptor Antagonists/pharmacology ; Serotonin 5-HT2 Receptor Antagonists/toxicity ; Structure-Activity Relationship ; Succinates/pharmacology ; Vasoconstriction/drug effects
    Chemical Substances Isoxazoles ; Platelet Aggregation Inhibitors ; Serotonin 5-HT2 Receptor Antagonists ; Succinates ; sarpogrelate (19P708E787)
    Language English
    Publishing date 2021-11-13
    Publishing country France
    Document type Comparative Study ; Journal Article
    ZDB-ID 392415-4
    ISSN 1950-6007 ; 0753-3322 ; 0300-0893
    ISSN (online) 1950-6007
    ISSN 0753-3322 ; 0300-0893
    DOI 10.1016/j.biopha.2021.112424
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Ud II Zs.198: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  7. Article ; Online: The Antidepressant-like Activity, Effects on Recognition Memory Deficits, Bioavailability, and Safety after Chronic Administration of New Dual-Acting Small Compounds Targeting Neuropsychiatric Symptoms in Dementia.

    Jastrzębska-Więsek, Magdalena / Kotańska, Magdalena / Grzeszczak, Aleksandra / Jaromin, Anna / Walczak, Maria / Partyka, Anna / Gdula-Argasińska, Joanna / Smolik, Magdalena / Zagórska, Agnieszka

    International journal of molecular sciences

    2022  Volume 23, Issue 19

    Abstract: This study aimed to extend the body of preclinical research on prototype dual-acting compounds combining the pharmacophores relevant for inhibiting cyclic nucleotide phosphodiesterase 10 (PDE10A) and serotonin 5- ... ...

    Abstract This study aimed to extend the body of preclinical research on prototype dual-acting compounds combining the pharmacophores relevant for inhibiting cyclic nucleotide phosphodiesterase 10 (PDE10A) and serotonin 5-HT
    MeSH term(s) Animals ; Antidepressive Agents/pharmacology ; Antidepressive Agents/therapeutic use ; Antioxidants ; Biological Availability ; Blood Glucose ; Brain-Derived Neurotrophic Factor/genetics ; Brain-Derived Neurotrophic Factor/metabolism ; Cholesterol ; Dementia ; Dizocilpine Maleate ; Humans ; Memory Disorders/drug therapy ; Nucleotides, Cyclic ; Phosphoric Diester Hydrolases ; RNA, Messenger ; Rats ; Serotonin/metabolism ; Triglycerides
    Chemical Substances Antidepressive Agents ; Antioxidants ; Blood Glucose ; Brain-Derived Neurotrophic Factor ; Nucleotides, Cyclic ; RNA, Messenger ; Triglycerides ; Serotonin (333DO1RDJY) ; Dizocilpine Maleate (6LR8C1B66Q) ; Cholesterol (97C5T2UQ7J) ; PDE10A protein, human (EC 3.1.4.-) ; Phosphoric Diester Hydrolases (EC 3.1.4.-)
    Language English
    Publishing date 2022-09-28
    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/ijms231911452
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  8. Article: Evaluation of the In Vitro Cytotoxic Activity of Caffeic Acid Derivatives and Liposomal Formulation against Pancreatic Cancer Cell Lines.

    Zaremba-Czogalla, Magdalena / Jaromin, Anna / Sidoryk, Katarzyna / Zagórska, Agnieszka / Cybulski, Marcin / Gubernator, Jerzy

    Materials (Basel, Switzerland)

    2020  Volume 13, Issue 24

    Abstract: Pancreatic cancer belongs to the most aggressive group of cancers, with very poor prognosis. Therefore, there is an important need to find more potent drugs that could deliver an improved therapeutic approach. In the current study we searched for ... ...

    Abstract Pancreatic cancer belongs to the most aggressive group of cancers, with very poor prognosis. Therefore, there is an important need to find more potent drugs that could deliver an improved therapeutic approach. In the current study we searched for selective and effective caffeic acid derivatives. For this purpose, we analyzed twelve compounds and evaluated their in vitro cytotoxic activity against two human pancreatic cancer cell lines, along with a control, normal fibroblast cell line, by the classic MTT assay. Six out of twelve tested caffeic acid derivatives showed a desirable effect. To improve the therapeutic efficacy of such active compounds, we developed a formulation where caffeic acid derivative (7) was encapsulated into liposomes composed of soybean phosphatidylcholine and DSPE-PEG
    Language English
    Publishing date 2020-12-19
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2487261-1
    ISSN 1996-1944
    ISSN 1996-1944
    DOI 10.3390/ma13245813
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  9. 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

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  10. Article ; Online: Liposomal formulation of a new antifungal hybrid compound provides protection against

    Jaromin, Anna / Zarnowski, Robert / Markowski, Adam / Zagórska, Agnieszka / Johnson, Chad J / Etezadi, Haniyeh / Kihara, Shinji / Mota-Santiago, Pablo / Nett, Jeniel E / Boyd, Ben J / Andes, David R

    Antimicrobial agents and chemotherapy

    2023  Volume 68, Issue 1, Page(s) e0095523

    Abstract: The newly emerged pathogen, ...

    Abstract The newly emerged pathogen,
    MeSH term(s) Humans ; Antifungal Agents/pharmacology ; Candida ; Candida auris ; Liposomes ; Microbial Sensitivity Tests ; Biofilms
    Chemical Substances Antifungal Agents ; Liposomes
    Language English
    Publishing date 2023-12-11
    Publishing country United States
    Document type Journal Article
    ZDB-ID 217602-6
    ISSN 1098-6596 ; 0066-4804
    ISSN (online) 1098-6596
    ISSN 0066-4804
    DOI 10.1128/aac.00955-23
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 809: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)
    Einzelsignatur: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

To top