The ability of bacterial species to resist antimicrobial agents is an increasingly serious and widespread phenomenon in the 21st century. In hospital settings, this issue is even more severe and evident, capable of causing hospital-acquired infections (HAIs), particularly nosocomial infections (NIs) mainly contracted from contaminated hospital equipment. The main multidrug-resistant bacteria (MDR) involved include methicillin-resistant Staphylococcus aureus (MRSA), extended-spectrum β-lactamase (ESBL) producers, and Mycobacterium tuberculosis. The growing number of resistances developed by bacterial species highlights the need to find new, effective, and non-toxic alternatives to known antibacterial substances, capable of interacting innovatively with the microorganisms in question. In this context, the conformational switching of azobenzene has allowed for the observation of variations in the potency and efficacy of existing drugs modified with azocompounds, as well as the ability to modulate drug activity, thereby reducing the possibility of drug resistance occurring.