Halogenation of Biotin Protein Ligase Inhibitors Improves Whole Cell Activity against <i>Staphylococcus aureus</i>

We report the synthesis and evaluation of 5-halogenated-1,2,3-triazoles as inhibitors of biotin protein ligase from <i>Staphylococcus aureus</i>. The halogenated compounds exhibit significantly improved antibacterial activity over their nonhalogenated counterparts. Importantly, the 5-fluoro-1,2,3-triazole compound <b>4c</b> displays antibacterial activity against <i>S. aureus</i> ATCC49775 with a minimum inhibitory concentration (MIC) of 8 μg/mL