Synonyms: compound 8 [PMID: 30803745]
Compound class:
Synthetic organic
Comment: TBAJ-587, an analogue of bedaquiline, was discovered at the University of Auckland following a lead optimization programme to identify novel members of the diarylquinolines class of antibacterial compounds [2]. TBAJ-587 has a more favourable ADME profile, lower risk of QT prolongation, and more potent antimycobacterial activity than bedaquiline [2].
See also our entry for TBAJ-876 that was identified in the same study. |
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References |
1. Courbon GM, Palme PR, Mann L, Richter A, Imming P, Rubinstein JL. (2023)
Mechanism of mycobacterial ATP synthase inhibition by squaramides and second generation diarylquinolines. EMBO J, 42 (15): e113687. [PMID:37377118] |
2. Sutherland HS, Tong AST, Choi PJ, Blaser A, Conole D, Franzblau SG, Lotlikar MU, Cooper CB, Upton AM, Denny WA et al.. (2019)
3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel. Bioorg Med Chem, 27 (7): 1292-1307. [PMID:30803745] |