ArticleJournal of medicinal chemistry2019
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 2 of them syntheses that pooled it.
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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.
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Who cites it
24 citing papers in PubMed, 2 syntheses or guidelines pooled it, 42 citations in OpenAlex.
- Updated annotation and meta-analysis of Brugia malayi transcriptomics data reveals consistent transcriptional profiles across time and space with some study-specific differences in adult female worm transcriptional profiles.PLoS neglected tropical diseases · 2024Pooled it
- A Meta-Analysis ofG3 (Bethesda, Md.) · 2020Pooled it
- Designing the Next Generation of Antibiotics: Structure, SAR, and Strategy in Medicinal Chemistry (2000-2025).Medicinal research reviews · 2026Review
- Targeting a microbiotaScience advances · 2024Article
- Exploiting thiol-functionalized benzosiloxaboroles for achieving diverse substitution patterns - synthesis, characterization and biological evaluation of promising antibacterial agents.RSC medicinal chemistry · 2024Article
- Assessing Boron-Pleuromutilin AN11251 for the Development of Antibacterial Agents.Molecules (Basel, Switzerland) · 2023Article
- Filariasis research - from basic research to drug development and novel diagnostics, over a decade of research at the Institute for Medical Microbiology, Immunology and Parasitology, Bonn, Germany.Frontiers in tropical diseases · 2023Article
- Dirofilariasis mouse models for heartworm preclinical research.Frontiers in microbiology · 2023Article
- Discovery of Substituted Di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as Novel Macrofilaricidal Compounds for the Treatment of Human Filarial Infections.Journal of medicinal chemistry · 2022Article
- Contemporary exploitation of natural products for arthropod-borne pathogen transmission-blocking interventions.Parasites & vectors · 2022Review
- Theoretical modeling and design of some pyrazolopyrimidine derivatives asIn silico pharmacology · 2022Article
- Current perspective of new anti-Wolbachial and direct-acting macrofilaricidal drugs as treatment strategies for human filariasis.GMS infectious diseases · 2022Review
- Molecular docking-based virtual screening, molecular dynamic simulation, and 3-D QSAR modeling of some pyrazolopyrimidine analogs as potent anti-filarial agents.In silico pharmacology · 2022Article
- Human filariasis-contributions of the Litomosoides sigmodontis and Acanthocheilonema viteae animal model.Parasitology research · 2021Review
- Heteroelement Analogues of Benzoxaborole and Related Ring Expanded Systems.Molecules (Basel, Switzerland) · 2021Review
- Organoboron Compounds: Effective Antibacterial and Antiparasitic Agents.Molecules (Basel, Switzerland) · 2021Review
- Merging Boron with Nitrogen-Oxygen Bonds: A Review on BON Heterocycles.Topics in current chemistry (Cham) · 2021Review
- Corallopyronin A for short-course anti-wolbachial, macrofilaricidal treatment of filarial infections.PLoS neglected tropical diseases · 2020Article
- Oxfendazole mediates macrofilaricidal efficacy against the filarial nematode Litomosoides sigmodontis in vivo and inhibits Onchocerca spec. motility in vitro.PLoS neglected tropical diseases · 2020Article
- Short-course quinazoline drug treatments are effective in the Litomosoides sigmodontis and Brugia pahangi jird models.International journal for parasitology. Drugs and drug resistance · 2020Article
Corrections and comments
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Authors and funding
34 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A series of pleuromutilins modified by introduction of a boron-containing heterocycle on C(14) of the polycyclic core are described. These analogs were found to be potent anti- Wolbachia antibiotics and, as such, may be useful in the treatment of filarial infections caused by Onchocerca volvulus, resulting in Onchocerciasis or river blindness, or Wuchereria bancrofti and Brugia malayi and related parasitic nematodes resulting in lymphatic filariasis. These two important neglected tropical diseases disproportionately impact patients in the developing world. The lead preclinical candidate compound containing 7-fluoro-6-oxybenzoxaborole (15, AN11251) was shown to have good in vitro anti- Wolbachia activity and physicochemical and pharmacokinetic properties providing high exposure in plasma. The lead was effective in reducing the Wolbachia load in filarial worms following oral administration to mice.
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Registered trials
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