Published on July 16, 2022 Updated on April 30, 2023

Giuseppina SABATINO

CNR, Istituto di Cristallografia, Catana, Italy
Visiting Scholar invited by research center BioCIS
Stays from 29th June to 19th July, 2022
Curriculum Vitae

The role of cyclopetides in medicinal chemistry
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.