The Development of New Methods for the Synthesis of PLP- Dependent Enzyme Inhibitors and Exploring Covalent Inhibition Potential of Bacterial Enzyme O-acetylserine Sulfhydrylase
Konstantinos Grammatoglou, Riga Technical University, Latvia
The Thesis is a collection of scientific publications focused on the synthesis of triF-Ala analogues as potential inhibitors of PLP-dependent enzyme OASS and the development of methods for the synthesis of PLP-dependent enzyme inhibitors. Direct C–H functionalization of tetrazoles was achieved using the turbo Grignard reagent (iPrMgClꞏLiCl). In addition, an electrochemically removable protecting group was used on tetrazoles, and the use of enantiomeric t-butanesulfinyl imines as electrophiles can deliver the corresponding addition products in diastereoselective manner.