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  1. Article ; Online: Development of benzodioxine-heteroarylpiperazines as highly potent and selective α2c antagonists.

    Wang, Shouming / Haikarainen, Anssi / Pohjakallio, Antti / Sipilä, Julius / Kaskinoro, Janne / Juhila, Satu / Jalava, Niina / Koskinen, Mikko / Vesajoki, Marja / Kumpulainen, Esa / Pystynen, Jarmo / Koskelainen, Tuula / Holm, Patrik / Din Belle, David

    Bioorganic & medicinal chemistry letters

    2022  Volume 77, Page(s) 129005

    Abstract: Here is reported the design and synthesis of a series of highly potent and selective α2C antagonists using benzodioxine methyl piperazine as a central scaffold by pharmacophoric analysis to improve the pharmacokinetics of suboptimal clinical candidate ... ...

    Abstract Here is reported the design and synthesis of a series of highly potent and selective α2C antagonists using benzodioxine methyl piperazine as a central scaffold by pharmacophoric analysis to improve the pharmacokinetics of suboptimal clinical candidate molecules.
    MeSH term(s) Receptors, Adrenergic, alpha-2
    Chemical Substances Receptors, Adrenergic, alpha-2
    Language English
    Publishing date 2022-09-26
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2022.129005
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: 2,3-Dihydrobenzo-dioxine piperidine derivatives as potent and selective α2c antagonists.

    Wang, Shouming / Haikarainen, Anssi / Pohjakallio, Antti / Sipilä, Julius / Kaskinoro, Janne / Juhila, Satu / Jalava, Niina / Koskinen, Mikko / Vesajoki, Marja / Kumpulainen, Esa / Pystynen, Jarmo / Koskelainen, Tuula / Holm, Patrik / Din Belle, David

    Bioorganic & medicinal chemistry letters

    2022  Volume 69, Page(s) 128783

    Abstract: In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective α2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule. ...

    Abstract In this manuscript, we report a series of benzodioxine methyl piperidine derivatives as highly potent and selective α2C antagonists by ligand design to improve the pharmacokinetics of a previous candidate molecule.
    MeSH term(s) Dioxins ; Piperidines/pharmacology ; Receptors, Adrenergic, alpha-2
    Chemical Substances Dioxins ; Piperidines ; Receptors, Adrenergic, alpha-2
    Language English
    Publishing date 2022-05-13
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2022.128783
    Database MEDical Literature Analysis and Retrieval System OnLINE

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