ArticleMolecules (Basel, Switzerland)2020
Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876-A Less Toxic and More Potent Analogue of Bedaquiline.
Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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10 citing papers in PubMed, 21 citations in OpenAlex.
- Factors influencing QT interval prolongation during rifampicin-resistant tuberculosis treatment: a multicenter real-world study from China.BMC infectious diseases · 2025Article
- The Kinetics of Bedaquiline Diffusion in Tuberculous Cavities Open a Window for the Emergence of Resistance.The Journal of infectious diseases · 2025Article
- Catalytic enantioselective total synthesis of antitubercular agents (-)-bedaquiline and (-)-sudapyridine enabled by dynamic kinetic resolution-asymmetric transfer hydrogenation.Chemical science · 2025Article
- Contribution of telacebec to novel drug regimens in a murine tuberculosis model.Antimicrobial agents and chemotherapy · 2025Article
- Relative Contributions of the Novel Diarylquinoline TBAJ-876 and its Active Metabolite to the Bactericidal Activity in a Murine Model of Tuberculosis.The Journal of infectious diseases · 2024Article
- Antibiotics in the clinical pipeline as of December 2022.The Journal of antibiotics · 2023Review
- Application of Enantioselective Sulfur Ylide Epoxidation to a Short Asymmetric Synthesis of Bedaquiline, a Potent Anti-Tuberculosis Drug.Organic letters · 2023Article
- Synthetic studies towards isomeric pyrazolopyrimidines as potential ATP synthesis inhibitors ofTetrahedron letters · 2022Article
- Comparative Efficacy of the Novel Diarylquinoline TBAJ-876 and Bedaquiline against a ResistantAntimicrobial agents and chemotherapy · 2021Article
- Chemical Classes Presenting Novel Antituberculosis Agents Currently in Different Phases of Drug Development: A 2010-2020 Review.Pharmaceuticals (Basel, Switzerland) · 2021Review
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Bedaquiline is a novel drug approved in 2012 by the FDA for treatment of drug-resistant tuberculosis (TB). Although it shows high efficacy towards drug-resistant forms of TB, its use has been limited by the potential for significant side effects. In particular, bedaquiline is a very lipophilic compound with an associated long terminal half-life and shows potent inhibition of the cardiac potassium hERG channel, resulting in QTc interval prolongation in humans that may result in cardiac arrhythmia. To address these issues, we carried out a drug discovery programme to develop an improved second generation analogue of bedaquiline. From this medicinal chemistry program, a candidate (TBAJ-876) has been selected to undergo further preclinical evaluation. During this evaluation, three major metabolites arising from TBAJ-876 were observed in several preclinical animal models. We report here our synthetic efforts to unequivocally structurally characterize these three metabolites through their independent directed synthesis.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.