ArticleAntimicrobial agents and chemotherapy2013
Chemobiosynthesis of new antimalarial macrolides.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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12 citing papers in PubMed.
- Benzoxaborole-modified azithromycins inhibit translation without inducingAntimicrobial agents and chemotherapy · 2026Article
- OSMAC Method to Assess Impact of Culture Parameters on Metabolomic Diversity and Biological Activity of Marine-Derived Actinobacteria.Marine drugs · 2023Article
- Quercetin inhibits Toxoplasma gondii tachyzoite proliferation and acts synergically with azithromycin.Parasites & vectors · 2023Article
- Prioritization of Microorganisms Isolated from the Indian Ocean SpongeMicroorganisms · 2023Article
- Targeting malaria parasites with novel derivatives of azithromycin.Frontiers in cellular and infection microbiology · 2022Article
- Article
- Engineering actinomycetes for biosynthesis of macrolactone polyketides.Microbial cell factories · 2019Review
- Targeting malaria parasite invasion of red blood cells as an antimalarial strategy.FEMS microbiology reviews · 2019Review
- Insights into the evolution and drug susceptibility of Babesia duncani from the sequence of its mitochondrial and apicoplast genomes.International journal for parasitology · 2019Article
- HSQC-TOCSY Fingerprinting-Directed Discovery of Antiplasmodial Polyketides from the Marine Ascidian-DerivedMarine drugs · 2018Article
- Macrolides and associated antibiotics based on similar mechanism of action like lincosamides in malaria.Malaria journal · 2016Article
- Macrolides rapidly inhibit red blood cell invasion by the human malaria parasite, Plasmodium falciparum.BMC biology · 2015Article
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Authors and funding
7 authors.
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Abstract
We have synthesized new derivatives of the macrolide antibiotics erythromycin and azithromycin. Novel deoxysugar moieties were attached to these standard antibiotics by biotransformation using a heterologous host. The resulting compounds were tested against several standard laboratory and clinically isolated bacterial strains. In addition, they were also tested in vitro against standard and drug-resistant strains of human malaria parasites (Plasmodium falciparum) and the liver stages of the rodent malaria parasite (Plasmodium berghei). Antibacterial activity of modified erythromycin and azithromycin showed no improvement over the unmodified macrolides, but the modified compounds showed a 10-fold increase in effectiveness after a short-term exposure against blood stages of malaria. The new compounds also remained active against azithromycin-resistant strains of P. falciparum and inhibited growth of liver-stage parasites at concentrations similar to those used for primaquine. Our findings show that malaria parasites have two distinct responses to macrolide antibiotics, one reflecting the prokaryotic origin of the apicoplast and a second, as-yet uncharacterized response that we attribute to the eukaryotic nature of the parasite. This is the first report for macrolides that target two different functions in the Plasmodium parasites.
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