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  1. Article ; Online: High ligand efficiency quinazoline compounds as novel A

    Bolteau, Raphaël / Duroux, Romain / Laversin, Amélie / Vreulz, Brandon / Shiriaeva, Anna / Stauch, Benjamin / Han, Gye Won / Cherezov, Vadim / Renault, Nicolas / Barczyk, Amélie / Ravez, Séverine / Coevoet, Mathilde / Melnyk, Patricia / Liberelle, Maxime / Yous, Saïd

    European journal of medicinal chemistry

    2022  Volume 241, Page(s) 114620

    Abstract: The past fifty years have been marked by the surge of neurodegenerative diseases. Unfortunately, current treatments are only symptomatic. Hence, the search for new and innovative therapeutic targets for curative treatments becomes a major challenge. ... ...

    Abstract The past fifty years have been marked by the surge of neurodegenerative diseases. Unfortunately, current treatments are only symptomatic. Hence, the search for new and innovative therapeutic targets for curative treatments becomes a major challenge. Among these targets, the adenosine A
    MeSH term(s) Adenosine A2 Receptor Antagonists/chemistry ; Adenosine A2 Receptor Antagonists/pharmacology ; Ligands ; Molecular Docking Simulation ; Purinergic P1 Receptor Antagonists/pharmacology ; Quinazolines/pharmacology ; Receptor, Adenosine A2A/chemistry ; Structure-Activity Relationship
    Chemical Substances Adenosine A2 Receptor Antagonists ; Ligands ; Purinergic P1 Receptor Antagonists ; Quinazolines ; Receptor, Adenosine A2A
    Language English
    Publishing date 2022-07-22
    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.2022.114620
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
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  2. Article ; Online: Synthesis and SAR Studies of Isoquinoline and Tetrahydroisoquinoline Derivatives as Melatonin Receptor Ligands.

    Ettaoussi, Mohamed / Laversin, Amélie / Vreulz, Brandon / Rami, Marouane / Lebegue, Nicolas / Delagrange, Philippe / Caignard, Daniel Henri / Melnyk, Patricia / Liberelle, Maxime / Yous, Saïd

    ChemMedChem

    2021  Volume 17, Issue 3, Page(s) e202100658

    Abstract: In our constant search for new successors of agomelatine, we report herein a new series of compounds resulting from bioisosteric modulation of the naphthalene ring. The isoquinoline and tetrahydroisoquinoline derivatives were synthesized and ... ...

    Abstract In our constant search for new successors of agomelatine, we report herein a new series of compounds resulting from bioisosteric modulation of the naphthalene ring. The isoquinoline and tetrahydroisoquinoline derivatives were synthesized and pharmacologically evaluated. This isosteric replacement of the naphthalene group of agomelatine has led to potent agonist and partial agonist compounds with nanomolar melatonergic binding affinities. Overall, the presence of a nitrogen atom was accompanied with a decrease in the binding affinity toward both MT
    MeSH term(s) Animals ; Cells, Cultured ; Cricetulus ; Dose-Response Relationship, Drug ; Humans ; Isoquinolines/chemistry ; Isoquinolines/metabolism ; Isoquinolines/pharmacology ; Ligands ; Molecular Docking Simulation ; Molecular Structure ; Receptors, Melatonin/agonists ; Structure-Activity Relationship
    Chemical Substances Isoquinolines ; Ligands ; Receptors, Melatonin ; isoquinoline (JGX76Y85M6)
    Language English
    Publishing date 2021-12-01
    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.202100658
    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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