Publié le 16 juillet 2022 Mis à jour le 30 avril 2023

Giuseppina SABATINO

CNR, Istituto di Cristallofraphia, Catane, Italie
Professeure invitée du laboratoire BioCIS
Séjour du 29 juin 2022 au 19 juillet 2022
Curriculum Vitae

Le rôle des cyclopetides en chimie médicale
Cyclopeptides represent an important class of starting materials in medicinal chemistry, their cyclic structures provide a predictable conformation, whose flexibility depends on the ring size. The reduced conformational flexibility of the cyclopeptides determine stability to metabolic degradation, enhancing the biological activity, the receptor selectivity, and bioavailability. Moreover, their constrained structure allows conformational investigations such as structure-activity relationship (SAR) studies. The cyclization step is the key step in the synthesis of the cyclopeptides due to the high tendency of the corresponding linear peptides to oligomerize. The purpose of this project is to investigate different strategies for cyclization of linear precursors into cyclic peptides both on resin and in solution.