Journal article
Halogenation of Biotin Protein Ligase Inhibitors Improves Whole Cell Activity against Staphylococcus aureus.
Ashleigh S Paparella, Kwang Jun Lee, Andrew J Hayes, Jiage Feng, Zikai Feng, Danielle Cini, Sonali Deshmukh, Grant W Booker, Matthew CJ Wilce, Steven W Polyak, Andrew D Abell
ACS Infectious Diseases | American Chemical Society | Published : 2018
Abstract
We report the synthesis and evaluation of 5-halogenated-1,2,3-triazoles as inhibitors of biotin protein ligase from Staphylococcus aureus. The halogenated compounds exhibit significantly improved antibacterial activity over their nonhalogenated counterparts. Importantly, the 5-fluoro-1,2,3-triazole compound 4c displays antibacterial activity against S. aureus ATCC49775 with a minimum inhibitory concentration (MIC) of 8 μg/mL.
Grants
Funding Acknowledgements
This work was supported by the National Health and Medical Research Council of Australia (application APP1068885). We are grateful to the Wallace and Carthew families for their financial support of this work.