"This dissertation focused on the development and advancement of methodology for accessing imidazoline scaffolds and other small heterocyclic molecules for biological evaluation. Past research within the Tepe group has correlated functionalized 2-imidazolines to proteasome modulation. Further diversification of the methodology for accessing these 2-imidazoline scaffolds, has allowed for the synthesis of a small library of analogs for SAR evaluation with the h20S proteasome. These finding were... Show more"This dissertation focused on the development and advancement of methodology for accessing imidazoline scaffolds and other small heterocyclic molecules for biological evaluation. Past research within the Tepe group has correlated functionalized 2-imidazolines to proteasome modulation. Further diversification of the methodology for accessing these 2-imidazoline scaffolds, has allowed for the synthesis of a small library of analogs for SAR evaluation with the h20S proteasome. These finding were used to further experimentally model and synthesize more efficacious 2-imidazoline derivates for proteasome modulation. The proteasome is responsible for the degradation of polyubiquitinated proteins in the cell, producing amino acids that can then be used for alternative cellular functions. The introducition of small heterocyclic molecules like 2- imidazolines, bind to the proteasome and lower is efficacy for protein digestion through modulation of its activity."--Page ii. Show less
