Nowadays, the C(sp2/sp3)-H activation reactions have been developed and established due to their great potentialities.1-2 Through them it is possible to carry out functionalization otherwise impracticable, enabling the activation of non-acidic unreactive CH bonds. Over the last years, the application of such reactions to complex molecules with biomedical relevance have appeared in the literature,3-4 although the activation of the less acidic and more unreactive C(sp3)-H bond remains a challenge. We set out to apply the 8-AQ directed C(sp3)-H activation reaction on complex molecules of biomedical interest, to insert additional chemical motifs that could be able to increase the inhibitory activity of the compounds toward a first selected target: β-secretase 1, a transmembrane protease involved in the formation of the amyloid plaques in the Alzheimer’s disease.

Probing bioactive motifs through C(sp3)-H activation for the development of protease inhibitors / Lorenzo Baldini, Elena Lenci, Andrea Trabocchi. - ELETTRONICO. - (2023), pp. 0-0. (Intervento presentato al convegno XLVII edition of “Attilio Corbella” International Summer School on Organic Sythesis (ISOS 2023)).

Probing bioactive motifs through C(sp3)-H activation for the development of protease inhibitors

Lorenzo Baldini;Elena Lenci;Andrea Trabocchi
2023

Abstract

Nowadays, the C(sp2/sp3)-H activation reactions have been developed and established due to their great potentialities.1-2 Through them it is possible to carry out functionalization otherwise impracticable, enabling the activation of non-acidic unreactive CH bonds. Over the last years, the application of such reactions to complex molecules with biomedical relevance have appeared in the literature,3-4 although the activation of the less acidic and more unreactive C(sp3)-H bond remains a challenge. We set out to apply the 8-AQ directed C(sp3)-H activation reaction on complex molecules of biomedical interest, to insert additional chemical motifs that could be able to increase the inhibitory activity of the compounds toward a first selected target: β-secretase 1, a transmembrane protease involved in the formation of the amyloid plaques in the Alzheimer’s disease.
2023
Book of Abstracts
XLVII edition of “Attilio Corbella” International Summer School on Organic Sythesis (ISOS 2023)
Lorenzo Baldini, Elena Lenci, Andrea Trabocchi
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1345272
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