ArticleACS medicinal chemistry letters2015
Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
What it found
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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.
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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.
- A Review of Antibacterial Candidates with New Modes of Action.ACS infectious diseases · 2024Review
- Antibiotics in the clinical pipeline as of December 2022.The Journal of antibiotics · 2023Review
- On drug discovery against infectious diseases and academic medicinal chemistry contributions.Beilstein journal of organic chemistry · 2022Article
- Antibiotics in the clinical pipeline in October 2019.The Journal of antibiotics · 2020Review
- Evolution and Antibacterial Evaluation of 8-Hydroxy-cycloberberine Derivatives as a Novel Family of Antibacterial Agents Against MRSA.Molecules (Basel, Switzerland) · 2019Article
- Article
- The Prodrug Approach: A Successful Tool for Improving Drug Solubility.Molecules (Basel, Switzerland) · 2015Review
Corrections and comments
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Authors and funding
18 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Benzimidazole 1 is the lead compound resulting from an antibacterial program targeting dual inhibitors of bacterial DNA gyrase and topoisomerase IV. With the goal of improving key drug-like properties, namely, the solubility and the formulability of 1, an effort to identify prodrugs was undertaken. This has led to the discovery of a phosphate ester prodrug 2. This prodrug is rapidly cleaved to the parent drug molecule upon both oral and intravenous administration. The prodrug achieved equivalent exposure of 1 compared to dosing the parent in multiple species. The prodrug 2 has improved aqueous solubility, simplifying both intravenous and oral formulation.
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Registered trials
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