In 1928, Alexander Fleming famously discovered what was to be the 'miracle drug', penicillin. Fast forward 90 years to the present day, we still find penicillin and its derivatives widely used in the clinic today. However, one major problem that is beginning to come to light is the widespread emergence of antibiotic resistance. As such, the World Health Organistation have declared research into novel antibiotics and diagnostic tools of paramount importance to our future. In search of a suitable drug target, Lipoteichoic acid Synthase (LtaS), an extracellular protein has been identified as a suitable candidate for a drug discovery campaign. Here, I describe our methodology for the identification and characterisation of small-molecule LtaS inhibitors that have been generated using a virtual screening approach. These compounds were able to act upon Gram-positive bacteria, such as methicillin-resistant Staphylococcus Aureus (MRSA), rendering them inactive and unable to survive.