ArticleBioorganic & medicinal chemistry2011
Synthesis and biological evaluation of new 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase.
Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed.
- Synthesis of Amino-Pharmaceuticals (Basel, Switzerland) · 2025Review
- Article
- Expanding the scope of novel 1,2,3-triazole derivatives as new antiparasitic drug candidates.RSC medicinal chemistry · 2023Article
- Article
- Article
- Bisphosphonate-Based Molecules as Potential New Antiparasitic Drugs.Molecules (Basel, Switzerland) · 2020Review
- Phosphonate and Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthases: A Structure-Guided Perspective.Frontiers in chemistry · 2020Review
- Synthesis and biological evaluation of 1-alkylaminomethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii.Bioorganic & medicinal chemistry · 2019Article
- Quantitative Structure-Activity Relationships for Structurally Diverse Chemotypes Having Anti-International journal of molecular sciences · 2019Article
- Antiparasitic Activity of Sulfur- and Fluorine-Containing Bisphosphonates against Trypanosomatids and Apicomplexan Parasites.Molecules (Basel, Switzerland) · 2017Article
- Review of Experimental Compounds Demonstrating Anti-Toxoplasma Activity.Antimicrobial agents and chemotherapy · 2016Review
- Synthetic Procedures Leading towards Aminobisphosphonates.Molecules (Basel, Switzerland) · 2016Review
- Triazole-based compound as a candidate to develop novel medicines to treat toxoplasmosis.Antimicrobial agents and chemotherapy · 2014Article
- Genetic profiling of the isoprenoid and sterol biosynthesis pathway genes of Trypanosoma cruzi.PloS one · 2014Article
- New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase.Bioorganic & medicinal chemistry · 2014Article
- Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents.European journal of medicinal chemistry · 2013Article
- Article
- 2-alkylaminoethyl-1,1-bisphosphonic acids are potent inhibitors of the enzymatic activity of Trypanosoma cruzi squalene synthase.Antimicrobial agents and chemotherapy · 2012Article
- Design, synthesis, calorimetry, and crystallographic analysis of 2-alkylaminoethyl-1,1-bisphosphonates as inhibitors of Trypanosoma cruzi farnesyl diphosphate synthase.Journal of medicinal chemistry · 2012Article
- 1-(Fluoroalkylidene)-1,1-bisphosphonic acids are potent and selective inhibitors of the enzymatic activity of Toxoplasma gondii farnesyl pyrophosphate synthase.Organic & biomolecular chemistry · 2012Article
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7 authors.
Funding
Abstract
The effect of long-chain 2-alkylaminoethyl-1,1-bisphosphonates against proliferation of the clinically more relevant form of Trypanosoma cruzi, the etiologic agent of American trypanosomiasis (Chagas' disease), and against tachyzoites of Toxoplasma gondii was investigated. Particularly, compound 26 proved to be an extremely potent inhibitor against the intracellular form of T. cruzi, exhibiting IC(50) values at the nanomolar range. This cellular activity was associated with a strong inhibition of the enzymatic activity of T. cruzi farnesyl diphosphate synthase (TcFPPS), which constitutes a valid target for Chagas' disease chemotherapy. Compound 26 was an effective agent against T. cruzi (amastigotes) exhibiting an IC(50) value of 0.67 μM, while this compound showed an IC(50) value of 0.81 μM against the target enzyme TcFPPS. This drug was less effective against the enzymatic activity of T. cruzi solanesyl diphosphate synthase TcSPPS showing an IC(50) value of 3.2 μM. Interestingly, compound 26 was also very effective against T. gondii (tachyzoites) exhibiting IC(50) values of 6.23 μM. This cellular activity was also related to the inhibition of the enzymatic activity towards the target enzyme TgFPPS (IC(50)=0.093 μM) As bisphosphonate-containing compounds are FDA-approved drugs for the treatment of bone resorption disorders, their potential low toxicity makes them good candidates to control different tropical diseases.
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