TBAJ-876 displays bedaquiline-like mycobactericidal potency without retaining the parental drug’s uncoupler activity

• Main Authors: Sarathy, Jickky Palmae, Ragunathan, Priya, Cooper, Christopher B., Upton, Anna M., Grüber, Gerhard, Dick, Thomas
• Other Authors: School of Biological Sciences
• Format: Article
• Language: English
• Published: 2020
• Subjects: Science::Biological sciences::Biochemistry; Science::Biological sciences::Molecular biology; TBAJ-876; Bedaquiline
• Online Access: https://hdl.handle.net/10356/138548
• Institution: Nanyang Technological University

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 pare...