ArticleAntimicrobial agents and chemotherapy2010
Activity of a trisubstituted pyrrole in inhibiting sporozoite invasion and blocking malaria infection.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 30 citations in OpenAlex.
- Versatile Imidazole Scaffold with Potent Activity against Multiple Apicomplexan Parasites.ACS infectious diseases · 2025Article
- Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase.Chembiochem : a European journal of chemical biology · 2022Article
- Plasmodium sporozoites on the move: Switching from cell traversal to productive invasion of hepatocytes.Molecular microbiology · 2021Review
- Malaria and tuberculosis as diseases of neglected populations: state of the art in chemotherapy and advances in the search for new drugs.Memorias do Instituto Oswaldo Cruz · 2020Review
- Review
- ABiology open · 2019Article
- Article
- Plasmodial Kinase Inhibitors: License to Cure?Journal of medicinal chemistry · 2018Article
- Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery.Antimicrobial agents and chemotherapy · 2017Article
- Progress in imaging methods: insights gained into Plasmodium biology.Nature reviews. Microbiology · 2017Review
- Invasion of hepatocytes by Plasmodium sporozoites requires cGMP-dependent protein kinase and calcium dependent protein kinase 4.Molecular microbiology · 2016Article
- Preassembled Single-Stranded RNA-Argonaute Complexes: A Novel Method to Silence Genes in Cryptosporidium.The Journal of infectious diseases · 2016Article
- Chemical probes of a trisubstituted pyrrole to identify its protein target(s) in Plasmodium sporozoites.Bioorganic & medicinal chemistry letters · 2013Article
- 4(1H)-Quinolones with liver stage activity against Plasmodium berghei.Antimicrobial agents and chemotherapy · 2013Article
- The role of cGMP signalling in regulating life cycle progression of Plasmodium.Microbes and infection · 2012Review
- Spatiotemporal and functional characterisation of the Plasmodium falciparum cGMP-dependent protein kinase.PloS one · 2012Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Malaria infection is initiated by Plasmodium sporozoites infecting the liver. Preventing sporozoite infection would block the obligatory first step of the infection and perhaps reduce disease severity. In addition, such an approach would decrease Plasmodium vivax hypnozoite formation and therefore disease relapses. Here we describe the activity of a trisubstituted pyrrole, 4-[2-(4-fluorophenyl)-5-(1-methylpiperidine-4-yl)-1H-pyrrol-3-yl] pyridine, in inhibiting motility, invasion, and consequently infection by P. berghei sporozoites. In tissue culture, the compound was effective within the first 3 h of sporozoite addition to HepG2 cells. In vivo, intraperitoneal administration of the compound significantly inhibited liver-stage parasitemia in P. yoelii sporozoite-infected mice and prevented the appearance of blood-stage parasites. P. berghei sporozoites lacking the parasite cGMP-dependent protein kinase, the primary target of the compound in erythrocyte-stage parasites, remained infectious to HepG2 cells and sensitive to the drug. These results suggest that the drug has an additional target(s) in sporozoites. We propose that drugs that inhibit sporozoite infection offer a feasible approach to malaria prophylaxis.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.