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- W2074709062 abstract "α-Fluorinated-1,1-bisphosphonic acids derived from fatty acids were designed, synthesized and biologically evaluated against Trypanosoma cruzi, the etiologic agent of Chagas disease, and against Toxoplasma gondii, the agent responsible for toxoplasmosis, and also towards the target parasitic enzymes farnesyl pyrophosphate synthase of T. cruzi (TcFPPS) and T. gondii (TgFPPS). Interestingly, 1-fluorononylidene-1,1-bisphosphonic acid (compound 43) proved to be an extremely potent inhibitor of the enzymatic activity of TgFPPS at the low nanomolar range, exhibiting an IC50 of 30 nM. This compound was two-fold more potent than risedronate (IC50 = 74 nM) that was taken as a positive control. This enzymatic activity was associated with a strong cell growth inhibition against tachyzoites of T. gondii, with an IC50 value of 2.7 μM." @default.
- W2074709062 created "2016-06-24" @default.
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- W2074709062 date "2012-01-01" @default.
- W2074709062 modified "2023-10-17" @default.
- W2074709062 title "1-(Fluoroalkylidene)-1,1-bisphosphonic acids are potent and selective inhibitors of the enzymatic activity of Toxoplasma gondii farnesyl pyrophosphate synthase" @default.
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- W2074709062 doi "https://doi.org/10.1039/c1ob06602a" @default.
- W2074709062 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3458512" @default.
- W2074709062 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22215028" @default.
- W2074709062 hasPublicationYear "2012" @default.
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