ArticleAntimicrobial agents and chemotherapy2014
Evaluation of the anti-Schistosoma mansoni activity of thiosemicarbazones and thiazoles.
Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 72 citations in OpenAlex.
- Schistosoma japonicum histone acetyltransferase 1 (SjHAT1): A novel anti-schistosomal drug target.PLoS pathogens · 2026Article
- Thiazole as a Promising Scaffold for the Treatment of Schistosomiasis: In Vitro and In Vivo Activity Against Different Developmental Stages ofPharmaceuticals (Basel, Switzerland) · 2026Article
- Use of Metabolomics Approach in the Discovery of Active Compounds from MacroalgaePharmaceutics · 2025Article
- Schistosomicidal effects of histone acetyltransferase inhibitors against Schistosoma japonicum juveniles and adult worms in vitro.PLoS neglected tropical diseases · 2024Article
- Stem cell-derived exosomes as a potential therapy for schistosomal hepatic fibrosis in experimental animals.Pathogens and global health · 2024Article
- Nature-Inspired Gallinamides Are Potent Antischistosomal Agents: Inhibition of the Cathepsin B1 Protease Target and Binding Mode Analysis.ACS infectious diseases · 2024Article
- Thiazole, Isatin and Phthalimide Derivatives TestedCurrent medicinal chemistry · 2024Review
- Targeting the Schistosoma mansoni nutritional mechanisms to design new antischistosomal compounds.Scientific reports · 2023Article
- Small change, big difference: A promising praziquantel derivative designated P96 with broad-spectrum antischistosomal activity for chemotherapy of schistosomiasis japonica.PLoS neglected tropical diseases · 2023Article
- Synergistic effect of combination chemotherapy with praziquantel and DW-3-15 for Schistosoma japonicum in vitro and in vivo.Parasites & vectors · 2021Article
- In vitro and in vivo evaluation of cnicin from blessed thistle (Centaurea benedicta) and its inclusion complexes with cyclodextrins against Schistosoma mansoni.Parasitology research · 2021Article
- Inhibition of 19S proteasome deubiquitinating activity in Schistosoma mansoni affects viability, oviposition, and structural changes.Parasitology research · 2020Article
- Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?RSC medicinal chemistry · 2020Review
- Assessment of the In Vitro Antischistosomal Activities of the Extracts and Compounds from Solidago Microglossa DC (Asteraceae) and Aristolochia Cymbifera Mart. & Zucc. (Aristolochiaceae).Evidence-based complementary and alternative medicine : eCAM · 2020Article
- In vitro and in vivo activities of DW-3-15, a commercial praziquantel derivative, against Schistosoma japonicum.Parasites & vectors · 2019Article
- In vitro activity of aryl-thiazole derivatives against Schistosoma mansoni schistosomula and adult worms.PloS one · 2019Article
- Phthalimido-thiazole as privileged scaffold: activity against immature and adult worms of Schistosoma mansoni.Parasitology research · 2018Article
- Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents.Revista do Instituto de Medicina Tropical de Sao Paulo · 2017Article
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Authors and funding
15 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Schistosomiasis is a chronic and debilitating disease caused by a trematode of the genus Schistosoma and affects over 207 million people. Chemotherapy is the only immediate recourse for minimizing the prevalence of this disease and involves predominately the administration of a single drug, praziquantel (PZQ). Although PZQ has proven efficacy, there is a recognized need to develop new drugs as schistosomicides since studies have shown that repeated use of this drug in areas of endemicity may cause a temporary reduction in susceptibility in isolates of Schistosoma mansoni. Hydrazones, thiosemicarbazones, phthalimides, and thiazoles are thus regarded as privileged structures used for a broad spectrum of activities and are potential candidates for sources of new drug prototypes. The present study determined the in vitro schistosomicidal activity of 10 molecules containing these structures. During the assays, parameters such motility and mortality, oviposition, morphological changes in the tegument, cytotoxicity, and immunomodulatory activity caused by these compounds were evaluated. The results showed that compounds formed of thiazole and phthalimide led to higher mortality of worms, with a significant decline in motility, inhibition of pairing and oviposition, and a mortality rate of 100% starting from 144 h of exposure. These compounds also stimulated the production of nitric oxide and tumor necrosis factor alpha (TNF-α), thereby demonstrating the presence of immunomodulatory activity. The phthalyl thiazole LpQM-45 caused significant ultrastructural alterations, with destruction of the tegument in both male and female worms. According to the present study, phthalyl thiazole compounds possess antischistosomal activities and should form the basis for future experimental and clinical trials.
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