ArticleAntimicrobial agents and chemotherapy2014
1,4-azaindole, a potential drug candidate for treatment of tuberculosis.
Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
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Who cites it
45 citing papers in PubMed.
- Translational Modeling of BTZ-043 to Predict Phase 2A Efficacy and Evaluate Drug-Drug Interactions With Bedaquiline, Pretomanid, and Linezolid in Murine Models.The Journal of infectious diseases · 2025Article
- Fighting Antimicrobial Resistance: Innovative Drugs in Antibacterial Research.Angewandte Chemie (International ed. in English) · 2025Review
- Revolutionizing tuberculosis treatment: Breakthroughs, challenges, and hope on the horizon.Acta pharmaceutica Sinica. B · 2025Review
- A Review of Antibacterial Candidates with New Modes of Action.ACS infectious diseases · 2024Review
- Bactericidal and sterilizing activity of novel regimens combining bedaquiline or TBAJ-587 with GSK2556286 and TBA-7371 in a mouse model of tuberculosis.Antimicrobial agents and chemotherapy · 2024Article
- Drug distribution and efficacy of the DprE1 inhibitor BTZ-043 in the C3HeB/FeJ mouse tuberculosis model.Antimicrobial agents and chemotherapy · 2023Article
- Unlocking New Prenylation Modes: Azaindoles as a New Substrate Class for Indole Prenyltransferases.ChemCatChem · 2023Article
- Antibiotics in the clinical pipeline as of December 2022.The Journal of antibiotics · 2023Review
- Mutations inAntimicrobial agents and chemotherapy · 2023Article
- Tuberculosis: Pathogenesis, Current Treatment Regimens and New Drug Targets.International journal of molecular sciences · 2023Review
- Assay development and inhibition of theMicrobiology (Reading, England) · 2023Article
- Advances in the design of combination therapies for the treatment of tuberculosis.Expert opinion on drug discovery · 2023Review
- Implications of Fragment-Based Drug Discovery in Tuberculosis and HIV.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Recent Advances of DprE1 Inhibitors againstACS omega · 2022Review
- Novel Regimens of Bedaquiline-Pyrazinamide Combined with Moxifloxacin, Rifabutin, Delamanid and/or OPC-167832 in Murine Tuberculosis Models.Antimicrobial agents and chemotherapy · 2022Article
- Review
- Screening biofilm eradication activity of ethanol extracts from foodstuffs: potent biofilm eradication activity of glabridin, a major flavonoid from licorice (Glycyrrhiza glabra), alone and in combination with ɛ-poly-L-lysine.World journal of microbiology & biotechnology · 2022Article
- Indole: A promising scaffold for the discovery and development of potential anti-tubercular agents.Current research in pharmacology and drug discovery · 2022Review
- Anti-tuberculosis drug developmentFrontiers in microbiology · 2022Review
- Comparative Analysis of Pharmacodynamics in the C3HeB/FeJ Mouse Tuberculosis Model for DprE1 Inhibitors TBA-7371, PBTZ169, and OPC-167832.Antimicrobial agents and chemotherapy · 2021Article
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Authors and funding
17 authors.
Funding
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Abstract
New therapeutic strategies against multidrug-resistant (MDR) and extensively drug-resistant (XDR) Mycobacterium tuberculosis are urgently required to combat the global tuberculosis (TB) threat. Toward this end, we previously reported the identification of 1,4-azaindoles, a promising class of compounds with potent antitubercular activity through noncovalent inhibition of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1). Further, this series was optimized to improve its physicochemical properties and pharmacokinetics in mice. Here, we describe the short-listing of a potential clinical candidate, compound 2, that has potent cellular activity, drug-like properties, efficacy in mouse and rat chronic TB infection models, and minimal in vitro safety risks. We also demonstrate that the compounds, including compound 2, have no antagonistic activity with other anti-TB drugs. Moreover, compound 2 shows synergy with PA824 and TMC207 in vitro, and the synergy effect is translated in vivo with TMC207. The series is predicted to have a low clearance in humans, and the predicted human dose for compound 2 is ≤1 g/day. Altogether, our data suggest that a 1,4-azaindole (compound 2) is a promising candidate for the development of a novel anti-TB drug.
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