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Title: TBAJ-876 displays bedaquiline-like mycobactericidal potency without retaining the parental drug’s uncoupler activity
Authors: Sarathy, Jickky Palmae
Ragunathan, Priya
Cooper, Christopher B.
Upton, Anna M.
Grüber, Gerhard
Dick, Thomas
Keywords: Science::Biological sciences::Biochemistry
Science::Biological sciences::Molecular biology
Issue Date: 2020
Source: Sarathy, J. P., Ragunathan, P., Cooper, C. B., Upton, A. M., Grüber, G., & Dick, T. (2020). TBAJ-876 displays bedaquiline-like mycobactericidal potency without retaining the parental drug’s uncoupler activity. Antimicrobial Agents and Chemotherapy, 64(2), e01540-19-. doi:10.1128/AAC.01540-19
Journal: Antimicrobial Agents and Chemotherapy
Abstract: The diarylquinoline F1FO-ATP synthase inhibitor bedaquiline (BDQ) displays protonophore activity. Thus, uncoupling electron transport from ATP synthesis appears to be a second mechanism of action of this antimycobacterial drug. Here, we show that the new BDQ analogue TBAJ-876 did not retain the parental drug’s protonophore activity. Comparative time-kill analyses revealed that both compounds exert the same bactericidal activity. These results suggest that the uncoupler activity is not required for the bactericidal activity of diarylquinolines.
ISSN: 0066-4804
DOI: 10.1128/AAC.01540-19
Rights: © 2020 Sarathy et al. This is an open-access article distributed under the terms of the Creative Commons Attribution 4.0 International license.
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SBS Journal Articles

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