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https://hdl.handle.net/2440/111395
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Type: | Journal article |
Title: | Halogenation of biotin protein ligase inhibitors improves whole cell activity against Staphylococcus aureus |
Author: | Paparella, A.S. Lee, K.J. Hayes, A.J. Feng, J. Feng, Z. Cini, D. Deshmukh, S. Booker, G.W. Wilce, M.C. Polyak, S.W. Abell, A.D. |
Citation: | ACS Infectious Diseases, 2018; 4(2):175-184 |
Publisher: | ACS Publications |
Issue Date: | 2018 |
ISSN: | 2373-8227 2373-8227 |
Statement of Responsibility: | Ashleigh S. Paparella, Kwang Jun Lee, Andrew J. Hayes, Jiage Feng, Zikai Feng, Danielle Cini, Sonali Deshmukh, Grant W. Booker, Matthew C. J. Wilce, Steven W. Polyak and Andrew D. Abell |
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 |
Rights: | © 2017 American Chemical Society |
DOI: | 10.1021/acsinfecdis.7b00134 |
Grant ID: | http://purl.org/au-research/grants/nhmrc/1068885 |
Published version: | http://dx.doi.org/10.1021/acsinfecdis.7b00134 |
Appears in Collections: | Aurora harvest 3 Medicine publications |
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