Medicinal Chemistry of Drugs with N-Oxide Functionalities

    March 2024 in “ Journal of Medicinal Chemistry
    Michelle Kobus, Timo Friedrich, Eilika Zorn, Nils Burmeister, Wolfgang Maison
    TLDR N-oxides are important in medicine for improving drug properties and targeting.
    Molecules with N-oxide functionalities are crucial in Medicinal Chemistry due to their roles as intermediates, prodrugs, drugs, or polymers. The N-oxide group enhances water solubility, reduces membrane permeability or immunogenicity, and exhibits unique redox reactivity important for drug targeting and cytotoxicity. Recent discoveries have expanded the understanding of these mechanisms, leading to a rapid increase in N-oxide applications in healthcare. This article summarizes the properties, synthesis, and current biomedical applications of N-oxides, highlighting the molecular mechanisms behind their biological activity.
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