Stereoselective synthesis and preliminary evaluation of (+)- and (-)-3-methyl-5-carboxy-thien-2-yl-glycine (3-MATIDA): Identification of (+)-3-MATIDA as a novel mGluR1 competitive antagonist

Gabriele Costantino, Maura Marinozzi, Emidio Camaioni, Benedetto Natalini, Iran Sarichelou, Fabrizio Micheli, Paolo Cavanni, Stefania Faedo, Christian Noe, Falvio Moroni, Roberto Pellicciari

    Veröffentlichungen: Beitrag in FachzeitschriftArtikelPeer Reviewed

    Abstract

    The synthesis of the (+)- and (-)-isomers of 3-methyl-5-carboxy-thyen-2-yl- glycine (3-MATIDA), heterocyle isosters of carboxyphenylglycines (CPGs), a known class of competitive metabotropic glutamate receptors, was accomplished by a stereoselective Ugi condensation. The two isomers were tested as potential rat mGluR1 ligand and the (+) isomer was found to be a moderately potent antagonist, while the (-) one was inactive. Π2003 Elsevier SAS. All rights reserved.
    OriginalspracheEnglisch
    Seiten (von - bis)93-99
    Seitenumfang7
    FachzeitschriftIl Farmaco
    Jahrgang59
    Ausgabenummer2
    PublikationsstatusVeröffentlicht - 2004

    ÖFOS 2012

    • 3012 Pharmazie, Pharmakologie, Toxikologie

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