Browsing by Author "Moglie, Yanina"

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    Bio-click chemistry: a bridge between biocatalysis and click chemistry
    (2022) Rodríguez Sánchez, Diego Fernando; Moglie, Yanina; Ramírez Sarmiento, César Antonio; Singh, Sachin Kumar; Dua, Kamal; Zacconi, Flavia C. M.
    The fields of click chemistry and biocatalysis have rapidly grown over the last two decades. The development of robust and active biocatalysts and the widespread use of straightforward click reactions led to significant interactions between these two fields. Therefore the name bio-click chemistry seems to be an accurate definition of chemoenzymatic reactions cooperating with click transformations. Bio-click chemistry can be understood as the approach towards molecules of high-value using a green and sustainable approach by exploiting the potential of biocatalytic enzyme activity combined with the reliable nature of click reactions. This review summarizes the principal bio-click chemistry reactions reported over the last two decades, with a special emphasis on small molecules. Contributions to the field of bio-click chemistry are manifold, but the synthesis of chiral molecules with applications in medicinal chemistry and sustainable syntheses will be especially highlighted.
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    Copper nanoparticles supported on zinc oxide as efficient catalyst for the N-Arylation of (Hetero)cyclic and acyclic amides
    (WILEY-V C H VERLAG GMBH, 2021) Moglie, Yanina; Mascaro, Evangelina; Zacconi, Flavia C. M.; Radivoy, Gabriel
    Copper nanoparticles (CuNPs) supported on ZnO are highly active and selective heterogeneous catalyst for the N-arylation of cyclic and acyclic amides (Golberg coupling). The reaction conditions are mild, featuring K3PO4 as a base and N,N'-dimethylethylendiamine (DMEDA) as ligand in refluxing acetonitrile. The CuNPs/ZnO catalyst can be recovered and reused in six cycles with only little loss of activity. The methodology can be successfully scaled up to gram scale without decreasing the catalytic activity.
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    Green by Design: Convergent Synthesis, Computational Analyses, and Activity Evaluation of New FXa Inhibitors Bearing Peptide Triazole Linking Units
    (2022) Rodriguez, Diego F.; Duran Osorio, Francisca; Duarte, Yorley; Olivares, Pedro; Moglie, Yanina; Dua, Kamal; Zacconi, Flavia C. M.
    Green chemistry implementation has led to promising results in waste reduction in the pharmaceutical industry. However, the early sustainable development of pharmaceutically active compounds and ingredients remains a considerable challenge. Herein, we wish to report a green synthesis of new pharmaceutically active peptide triazoles as potent factor Xa inhibitors, an important drug target associated with the treatment of diverse cardiovascular diseases. The new inhibitors were synthesized in three steps, featuring cycloaddition reactions (high atom economy), microwave-assisted organic synthesis (energy efficiency), and copper nanoparticle catalysis, thus featuring Earth-abundant metals. The molecules obtained showed FXa inhibition, with IC50-values as low as 17.2 mu M and no associated cytotoxicity in HEK293 and HeLa cells. These results showcase the environmental potential and chemical implications of the applied methodologies for the development of new molecules with pharmacological potential.