Inhibitors of the folate pathway enzymes HPPK and DHPS DENNISMATTHEW LLOYD 2017 Antibiotic resistance is one of the most significant healthcare challenges of the current century, and novel drugs are of grave necessity. This thesis focuses on the development of such drugs. By targeting proteins that are present in bacteria, yet absent in humans, the risk of drug side-effects is minimised. Additionally, when an antibiotic acts on multiple proteins within a cell, the likelihood of resistance developing to that antibiotic may be reduced. A compound that possesses both these attributes is selected for development — the derived compounds are a significant improvement and represent promising leads for novel and effective therapeutics.