606970-75-6Relevant academic research and scientific papers
Salicylic Acid Derivatives Inhibit Oxalate Production in Mouse Hepatocytes with Primary Hyperoxaluria Type 1
Moya-Garzón, María Dolores,Martín Higueras, Cristina,Pe?alver, Pablo,Romera, Manuela,Fernandes, Miguel X.,Franco-Montalbán, Francisco,Gómez-Vidal, José A.,Salido, Eduardo,Díaz-Gavilán, Mónica
, p. 7144 - 7167 (2018)
Primary hyperoxaluria type 1 (PH1) is a rare life-threatening genetic disease related to glyoxylate metabolism and characterized by accumulation of calcium oxalate crystals. Current therapies involve hepatic and/or renal transplantation, procedures that have significant morbidity and mortality and require long-term immunosuppression. Thus, a pharmacological treatment is urgently needed. We introduce here an unprecedented activity of salicylic acid derivatives as agents capable of decreasing oxalate output in hyperoxaluric hepatocytes at the low micromolar range, which means a potential use in the treatment of PH1. Though correlation of this phenotypic activity with glycolate oxidase (GO) inhibition is still to be verified, most of the salicylic acids described here are GO inhibitors with IC50 values down to 3 μM. Binding mode of salicylic acids inside GO has been studied using in silico methods, and preliminary structure-activity relationships have been established. The drug-like structure and ease of synthesis of our compounds make them promising hits for structural optimization.
Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase
Xie, Yuli,Liu, Yidong,Gong, Gangli,Rinderspacher, Alison,Deng, Shi-Xian,Smith, Deborah H.,Toebben, Udo,Tzilianos, Effie,Branden, Lars,Vidovic, Dusica,Chung, Caty,Schuerer, Stephan,Tautz, Lutz,Landry, Donald W.
, p. 2840 - 2844 (2008/12/21)
We report here a class of thiazolidine-2,4-diones and 2-thioxothiazolidin-4-ones as potent inhibitors of the lymphoid specific tyrosine phosphatase (Lyp) identified from high throughput screens. Chemical modification by incorporating the known phosphotyro
