ArticleBioorganic & medicinal chemistry letters2016
Synthesis and evaluation of pretomanid (PA-824) oxazolidinone hybrids.
Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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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.
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Who cites it
7 citing papers in PubMed, 35 citations in OpenAlex.
- Prospectively predicting BPaMZ phase IIb/III trial outcomes using a translational mouse-to-human platform.Antimicrobial agents and chemotherapy · 2024Trial
- Translational predictions of phase 2a first-in-patient efficacy studies for antituberculosis drugs.The European respiratory journal · 2023Article
- Synthesis of 2-(6-substituted quinolin-4-yl)-1-alkoxypropan-2-ol as potential antimycobacterial agents.Chemicke zvesti · 2023Article
- Article
- Combination Therapy to Kill Mycobacterium tuberculosis in Its Nonreplicating Persister Phenotype.Antimicrobial agents and chemotherapy · 2022Article
- A validated liquid chromatography tandem mass spectrometry assay for the analysis of pretomanid in plasma samples from pulmonary tuberculosis patients.Journal of pharmaceutical and biomedical analysis · 2021Article
- Recent Progress in the Discovery and Development of 2-Nitroimidazooxazines and 6-Nitroimidazooxazoles to Treat Tuberculosis and Neglected Tropical Diseases.Molecules (Basel, Switzerland) · 2020Review
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Pretomanid (PA-824) is an important nitroimidazole antitubercular agent in late stage clinical trials. However, pretomanid is limited by poor solubility and high protein binding, which presents opportunities for improvement in its physiochemical properties. Conversely, the oxazolidinone linezolid has excellent physicochemical properties and has recently shown impressive activity for the treatment of drug resistant tuberculosis. In this study we explore if incorporation of the outer ring elements found in first and second generation oxazolidinones into the nitroimidazole core of pretomanid can be used to improve its physicochemical and antitubercular properties. The synthesis of pretomanid outer oxazolidinone ring hybrids was successfully performed producing hybrids that maintained antitubercular activity and had improved in vitro physicochemical properties. Three lead compounds were identified and evaluated in a chronic model of tuberculosis infection in mice. However, the compounds lacked efficacy suggesting that portions of PA-824 tail not found in the hybrid molecules are required for in vivo efficacy.
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