Substituted benzoxaboroles whose structure comprises Formula (III), wherein R3 is selected from —CH3, —CII2CII3, —CII2═CII2, —CII2CII2CII3, —CH(CH3)2, —CH2CH2═CH2, and cyclopropyl, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, and —CH(CH3)2; compositions containing such compounds, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.