ArticleScientific reports2017
Novel giardicidal compounds bearing proton pump inhibitor scaffold proceeding through triosephosphate isomerase inactivation.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 25 citations in OpenAlex.
- Targeting G6PD with Benzimidazole and Thiazole Derivatives SuppressesInternational journal of molecular sciences · 2025Article
- Nitazoxanide Analogs: Synthesis, In Vitro Giardicidal Activity, and Effects onInternational journal of molecular sciences · 2025Article
- In Vitro Evaluation of Esters of Quinoxaline-1,4-di-Pharmaceuticals (Basel, Switzerland) · 2025Article
- Effect of Trichomonacide 6-Nitro-1International journal of molecular sciences · 2024Article
- Fused Enzyme Glucose-6-Phosphate Dehydrogenase::6-Phosphogluconolactonase (G6PD::6PGL) as a Potential Drug Target inMicroorganisms · 2024Review
- Pyridyl Methylsulfinyl Benzimidazole Derivatives as Promising Agents againstMolecules (Basel, Switzerland) · 2022Article
- An Overview of Mucosa-Associated Protozoa: Challenges in Chemotherapy and Future Perspectives.Frontiers in cellular and infection microbiology · 2022Review
- Anti-infective properties of proton pump inhibitors: perspectives.International microbiology : the official journal of the Spanish Society for Microbiology · 2022Article
- Influence of Proton Pump Inhibitors and Histamine Receptor 2 Antagonists on Blastocystis ST3 and Selected Microorganisms of Intestinal Microbiota In Vitro.Clinical and translational gastroenterology · 2021Article
- Enhanced Antigiardial Effect of Omeprazole Analog Benzimidazole Compounds.Molecules (Basel, Switzerland) · 2020Article
- Metronidazole and Secnidazole Carbamates: Synthesis, Antiprotozoal Activity, and Molecular Dynamics Studies.Molecules (Basel, Switzerland) · 2020Article
- Crystal structures of Triosephosphate Isomerases from Taenia solium and Schistosoma mansoni provide insights for vaccine rationale and drug design against helminth parasites.PLoS neglected tropical diseases · 2020Article
- Gene Cloning, Recombinant Expression, Characterization, and Molecular Modeling of the Glycolytic Enzyme Triosephosphate Isomerase fromMicroorganisms · 2019Article
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Authors and funding
16 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Giardiasis is a worldwide parasitic disease that affects mainly children and immunosuppressed people. Side effects and the emergence of resistance over current used drugs make imperative looking for new antiparasitics through discovering of new biological targets and designing of novel drugs. Recently, it has determined that gastric proton-pump inhibitors (PPI) have anti-giardiasic activity. The glycolytic enzyme, triosephosphate isomerase (GlTIM), is one of its potential targets. Therefore, we employed the scaffold of PPI to design new compounds aimed to increase their antigiardial capacity by inactivating GlTIM. Here we demonstrated that two novel PPI-derivatives (BHO2 and BHO3), have better anti-giardiasic activity than omeprazole in concentrations around 120-130 µM, without cytotoxic effect on mammal cell cultures. The derivatives inactivated GlTIM through the chemical modification of Cys222 promoting local structural changes in the enzyme. Furthermore, derivatives forms adducts linked to Cys residues through a C-S bond. We demonstrated that PPI can be used as scaffolds to design better antiparasitic molecules; we also are proposing a molecular mechanism of reaction for these novel derivatives.
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