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. 2018 Feb 9;4(2):175-184.
doi: 10.1021/acsinfecdis.7b00134. Epub 2017 Nov 16.

Halogenation of Biotin Protein Ligase Inhibitors Improves Whole Cell Activity against Staphylococcus aureus

Ashleigh S Paparella  1 , Kwang Jun Lee  2 , Andrew J Hayes  1 , Jiage Feng  2   3 , Zikai Feng  1 , Danielle Cini  4 , Sonali Deshmukh  1 , Grant W Booker  1 , Matthew C J Wilce  4 , Steven W Polyak  1 , Andrew D Abell  2   3
Affiliations

Halogenation of Biotin Protein Ligase Inhibitors Improves Whole Cell Activity against Staphylococcus aureus

Ashleigh S Paparella et al. ACS Infect Dis. .

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.

Keywords: Staphylococcus aureus; antibiotic; biotin protein ligase; enzyme inhibitor.

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