Abstract

To develop effective agents to combat bacterial infections, a series of thiourea derivatives (TDs) were prepared and their antibacterial activities were evaluated. Our results showed thatTD4exerted the most potent antibacterial activity against a number ofStaphylococcus aureus(S. aureus), including the methicillin-resistantStaphylococcus aureus(MRSA),Staphylococcus epidermidisandEnterococcus faecalisstrains, with the minimum inhibitory concentration (MIC) at 2–16 µg/mL. It inhibited the MRSA growth curve in a dose-dependent manner and reduced the colony formation unit in 4× MIC within 4 h. Under the transmission electron microscope,TD4disrupted the integrity of MRSA cell wall. Additionally, it reduced the infective lesion size and the bacterial number in the MRSA-induced infection tissue of mice and possessed a good drug likeness according to the Lipinski rules. Our results indicate thatTD4is a potential lead compound for the development of novel antibacterial agent against the MRSA infection.Keywords:thiourea;Staphylococcus aureus;drug resistance;antibacterial activity;infection