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  1. Article ; Online: Development of Novel Isoindolone-Based Compounds against Trypanosoma brucei rhodesiense.

    Silva, Daniel G / Feijens, Pim-Bart / Hendrickx, Rik / Matheeussen, An / Grey, Lucie / Caljon, Guy / Maes, Louis / Emery, Flavio S / Junker, Anna

    ChemistryOpen

    2021  Volume 10, Issue 9, Page(s) 922–927

    Abstract: This study identified the isoindolone ring as a scaffold for novel agents against Trypanosoma brucei rhodesiense and explored the structure-activity relationships of various aromatic ring substitutions. The compounds were evaluated in an integrated in ... ...

    Abstract This study identified the isoindolone ring as a scaffold for novel agents against Trypanosoma brucei rhodesiense and explored the structure-activity relationships of various aromatic ring substitutions. The compounds were evaluated in an integrated in vitro screen. Eight compounds exhibited selective activity against T. b. rhodesiense (IC
    MeSH term(s) Animals ; Cell Line ; Drug Stability ; Female ; Humans ; Isoindoles/chemical synthesis ; Isoindoles/metabolism ; Isoindoles/pharmacology ; Isoindoles/toxicity ; Mice ; Microsomes, Liver/metabolism ; Molecular Structure ; Parasitic Sensitivity Tests ; Solubility ; Structure-Activity Relationship ; Trypanocidal Agents/chemical synthesis ; Trypanocidal Agents/metabolism ; Trypanocidal Agents/pharmacology ; Trypanocidal Agents/toxicity ; Trypanosoma brucei rhodesiense/drug effects
    Chemical Substances Isoindoles ; Trypanocidal Agents
    Language English
    Publishing date 2021-09-23
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2655605-4
    ISSN 2191-1363 ; 2191-1363
    ISSN (online) 2191-1363
    ISSN 2191-1363
    DOI 10.1002/open.202100180
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Imaging of K

    Thale, Insa / Maskri, Sarah / Grey, Lucie / Todesca, Luca Matteo / Budde, Thomas / Maisuls, Ivan / Strassert, Cristian A / Koch, Oliver / Schwab, Albrecht / Wünsch, Bernhard

    ChemMedChem

    2022  Volume 18, Issue 2, Page(s) e202200551

    Abstract: ... The ... ...

    Abstract The Ca
    MeSH term(s) Male ; Mice ; Humans ; Animals ; Carcinoma, Non-Small-Cell Lung ; Lung Neoplasms/diagnostic imaging ; Lung Neoplasms/pathology ; Fluorescent Dyes ; Cryoelectron Microscopy ; Positron-Emission Tomography ; Cell Line, Tumor
    Chemical Substances senicapoc (TS6G201A6Q) ; Fluorescent Dyes
    Language English
    Publishing date 2022-11-22
    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.202200551
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6280: Show issues Location:
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  3. Article ; Online: In vitro

    Bechthold, Elena / Grey, Lucie / Diamant, Emil / Schmidt, Judith / Steigerwald, Ruben / Zhao, Fabao / Hansen, Kasper B / Bunch, Lennart / Clausen, Rasmus P / Wünsch, Bernhard

    Biological chemistry

    2022  Volume 404, Issue 4, Page(s) 255–265

    Abstract: The GluN2C subunit exists predominantly, but not exclusively in NMDA receptors within the cerebellum. Antagonists such as UBP1700 and positive allosteric modulators including PYD-106 and 3-acylamino-2-aminopropionic acid derivatives such as UA3-10 (( ...

    Abstract The GluN2C subunit exists predominantly, but not exclusively in NMDA receptors within the cerebellum. Antagonists such as UBP1700 and positive allosteric modulators including PYD-106 and 3-acylamino-2-aminopropionic acid derivatives such as UA3-10 ((
    MeSH term(s) Mice ; Humans ; Animals ; Swine ; Receptors, N-Methyl-D-Aspartate/metabolism ; Prodrugs/pharmacology ; Prodrugs/chemistry ; Esters ; Binding Sites ; Esterases/metabolism
    Chemical Substances Receptors, N-Methyl-D-Aspartate ; Prodrugs ; Esters ; Esterases (EC 3.1.-)
    Language English
    Publishing date 2022-11-25
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
    ZDB-ID 1334659-3
    ISSN 1437-4315 ; 1431-6730 ; 1432-0355
    ISSN (online) 1437-4315
    ISSN 1431-6730 ; 1432-0355
    DOI 10.1515/hsz-2022-0229
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Synthesis of tropane-based σ

    Bechthold, Elena / Schreiber, Julian A / Ritter, Nadine / Grey, Lucie / Schepmann, Dirk / Daniliuc, Constantin / González-Cano, Rafael / Nieto, Francisco Rafael / Seebohm, Guiscard / Wünsch, Bernhard

    European journal of medicinal chemistry

    2022  Volume 230, Page(s) 114113

    Abstract: Following the concept of conformational restriction to obtain high affinity ... ...

    Abstract Following the concept of conformational restriction to obtain high affinity σ
    Language English
    Publishing date 2022-01-13
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2022.114113
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.B 784: Show issues Location:
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  5. Article ; Online: Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists.

    Patberg, Marius / Isaak, Andreas / Füsser, Friederike / Ortiz Zacarías, Natalia V / Vinnenberg, Laura / Schulte, Janine / Michetti, Lucia / Grey, Lucie / van der Horst, Cas / Hundehege, Petra / Koch, Oliver / Heitman, Laura H / Budde, Thomas / Junker, Anna

    European journal of medicinal chemistry

    2021  Volume 226, Page(s) 113838

    Abstract: The P2X7 receptor (P2X7R) stands out among the purinergic receptors due to its strong involvement in the regulation of tumor growth and metastasis formation as well as in innate immune responses and afferent signal transmission. Numerous studies have ... ...

    Abstract The P2X7 receptor (P2X7R) stands out among the purinergic receptors due to its strong involvement in the regulation of tumor growth and metastasis formation as well as in innate immune responses and afferent signal transmission. Numerous studies have pointed out the beneficial effects of P2X7R antagonism for the treatment of a variety of cancer types, inflammatory diseases, and chronic pain. Herein we describe the development of novel P2X7R antagonists, incorporating piperazine squaric diamides as a central element. Besides improving the antagonists' potency from pIC
    MeSH term(s) Cyclobutanes/chemical synthesis ; Cyclobutanes/chemistry ; Cyclobutanes/pharmacology ; Diamide/chemical synthesis ; Diamide/chemistry ; Diamide/pharmacology ; Dose-Response Relationship, Drug ; HEK293 Cells ; Humans ; Molecular Structure ; Piperazine/chemical synthesis ; Piperazine/chemistry ; Piperazine/pharmacology ; Purinergic P2X Receptor Antagonists/chemical synthesis ; Purinergic P2X Receptor Antagonists/chemistry ; Purinergic P2X Receptor Antagonists/pharmacology ; Receptors, Purinergic P2X/metabolism ; Structure-Activity Relationship ; Tumor Cells, Cultured
    Chemical Substances Cyclobutanes ; Purinergic P2X Receptor Antagonists ; Receptors, Purinergic P2X ; Diamide (10465-78-8) ; Piperazine (1RTM4PAL0V) ; squaric acid (SVR9D0VODW)
    Language English
    Publishing date 2021-09-16
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2021.113838
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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