ArticleBioorganic & medicinal chemistry2019
Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
Article in Bioorganic & medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
15 citing papers in PubMed, 51 citations in OpenAlex.
- Cytotoxicity and Antimicrobial Activity of GaMF1 Analogs.ChemMedChem · 2026Article
- Article
- Formulation and optimisation of bedaquiline nanoemulsions for the potential treatment of multi drug resistant tuberculosis in paediatrics using quality by design.Scientific reports · 2024Article
- Review
- New Quinoline-Urea-Benzothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Synthetic studies towards isomeric pyrazolopyrimidines as potential ATP synthesis inhibitors ofTetrahedron letters · 2022Article
- Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit.RSC medicinal chemistry · 2021Article
- Targeting the menaquinol binding loop of mycobacterial cytochrome bd oxidase.Molecular diversity · 2021Article
- The Unique C-Terminal Extension of Mycobacterial F-ATP Synthase Subunit α Is the Major Contributor to Its Latent ATP Hydrolysis Activity.Antimicrobial agents and chemotherapy · 2020Article
- SAR Analysis of Small Molecules Interfering with Energy-Metabolism inPharmaceuticals (Basel, Switzerland) · 2020Review
- TBAJ-876, a 3,5-Dialkoxypyridine Analogue of Bedaquiline, Is Active against Mycobacterium abscessus.Antimicrobial agents and chemotherapy · 2020Article
- Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876-A Less Toxic and More Potent Analogue of Bedaquiline.Molecules (Basel, Switzerland) · 2020Article
- TBAJ-876 Displays Bedaquiline-Like Mycobactericidal Potency without Retaining the Parental Drug's Uncoupler Activity.Antimicrobial agents and chemotherapy · 2020Article
- Re-Understanding the Mechanisms of Action of the Anti-Mycobacterial Drug Bedaquiline.Antibiotics (Basel, Switzerland) · 2019Review
- TBAJ-876 Retains Bedaquiline's Activity against Subunits c and ε ofAntimicrobial agents and chemotherapy · 2019Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The ATP-synthase inhibitor bedaquiline is effective against drug-resistant tuberculosis but is extremely lipophilic (clogP 7.25) with a very long plasma half-life. Additionally, inhibition of potassium current through the cardiac hERG channel by bedaquiline, is associated with prolongation of the QT interval, necessitating cardiovascular monitoring. Analogues were prepared where the naphthalene C-unit was replaced with substituted pyridines to produce compounds with reduced lipophilicity, anticipating a reduction in half-life. While there was a direct correlation between in vitro inhibitory activity against M. tuberculosis (MIC
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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.