Design, synthesis, and application of modular building blocks for structural investigations of functional peptides

The present work focuses on five objective targets as listed below: 1. Design of disubstituted [1,2,3]-triazolyl-comprising molecular blocks as peptide backbone mimics with locked amide conformation; 2. Development of a valid synthetic approach towards the mentioned triazolyl surrogates with focus on their application in Fmoc-based SPPS; 3. Study of the structure-activity relationship in peptidic molecules using the developed triazolyl blocks on two model systems: a) the potent protease inhibitor sunflower trypsin inhibitor 1 (SFTI-1[1,14]) and b) a peptide-based enzyme maquette of nickel superoxide dismutase (Ni(m7-NH2)); 4. Study of the structural properties of triazolyl patterns in peptidic molecules using molecular dynamic simulations; 5. Development of a valuable system towards the study of PHIP effects in biomolecules based on model peptides comprising an unsaturated alkyne moiety in their side chains.