Disclosed herein are novel uses of avenaciolide derivatives and the preparation method of producing the same. The avenaciolide derivatives may suppress or inhibit the growth of gram-positive bacteria, including the notorious methicillin-resistant Staphylococcus aureus. Accordingly, the avenaciolides derivatives are potential lead compounds for the development of next generation antibiotics for the treatment of disease and/or disorders related to infection caused by gram-positive bacteria.
