A light-activatable antibiotic with high activation efficiency and uncompromised bactericidal potency in the activated state

Achieving activatable antibiotics represents one promising solution to tackle the occurrence of side effects, one major issue now plaguing antibiotic usage in collagen-based biomaterials. Despite considerable effort, however, rationale design of activatable antibiotics that display high activation efficiency and uncompromised bactericidal potency in the activated state remains difficult. Here, we demonstrate a design principle that helps to address this challenge. This strategy differs from previous attempts by underscoring photolytic removal of a functionality directly conjugated to the pharmacophore of an antibiotic, enabling not only an activation efficiency significantly improved beyond previous light-activatable antibiotics, but also bactericidal activity in the activated state as potent as the parent drug.