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Propargylamine: an important moiety in drug discovery

    Aitor Carneiro

    CIQUP-IMS/Department of Chemistry & Biochemistry, Faculty of Sciences, University of Porto, Rua do Campo Alegre 687, Porto, 4169-007, Portugal

    ,
    Eugenio Uriarte

    Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, Santiago de Compostela, 15782, Spain

    Instituto de Ciencias Químicas Aplicadas, Universidad Autónoma de Chile, Santiago, 7500912, Chile

    ,
    Fernanda Borges

    CIQUP-IMS/Department of Chemistry & Biochemistry, Faculty of Sciences, University of Porto, Rua do Campo Alegre 687, Porto, 4169-007, Portugal

    &
    Maria João Matos

    *Author for correspondence: Tel.: +34 881 814 936;

    E-mail Address: maria.matos@fc.up.pt

    ,

    E-mail Address: mariajoao.correiapinto@usc.es

    CIQUP-IMS/Department of Chemistry & Biochemistry, Faculty of Sciences, University of Porto, Rua do Campo Alegre 687, Porto, 4169-007, Portugal

    Departamento de Química Orgánica, Facultade de Farmacia, Universidade de Santiago de Compostela, Santiago de Compostela, 15782, Spain

    Published Online:https://doi.org/10.4155/fmc-2022-0243

    Propargylamine is a chemical moiety whose properties have made it a widely distributed group within the fields of medicinal chemistry and chemical biology. Its particular reactivity has traditionally popularized the preparation of propargylamine derivatives using a large variety of synthetic strategies, which have facilitated the access to these compounds for the study of their biomedical potential. This review comprehensively covers and analyzes the applications that propargylamine-based derivatives have achieved in the drug discovery field, both from a medicinal chemistry perspective and from a chemical biology-oriented approach. The principal therapeutic fields where propargylamine-based compounds have made an impact are identified, and a discussion of their influence and growing potential is included.

    Graphical abstract

    Tweetable abstract

    Propargylamine derivatives are commonly present in various areas of #drugdiscovery. In this new @fsgfmc review article, scientists @aitorcarneiro and @mariacmatos from @UPorto and @UniversidadeUSC discuss the reasons underlying recent uses and applications of these compounds.

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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