1261968-90-4Relevant academic research and scientific papers
COMPOUNDS FOR THE TREATMENT OF DISEASES CAUSED BY OXALATE ACCUMULATION
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Paragraph 0085; 0088, (2020/02/04)
The present invention relates to the use of derivatives of salicylic acid for the treatment of diseases or conditions linked to GO and/or PRODH2 enzyme activity, in particular diseases linked to an excess of oxalate, and for the treatment of patients with
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
supporting information, p. 7144 - 7167 (2018/08/01)
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.
Synthesis and biological evaluation of salicylate-based compounds as a novel class of methionine aminopeptidase inhibitors
Wang, Wen-Long,Chai, Sergio C.,Ye, Qi-Zhuang
scheme or table, p. 7151 - 7154 (2012/01/06)
A series of salicylate-based compounds were designed and synthesized based on the simple function group replacement from our previously reported catechol-containing inhibitors of methionine aminopeptidase (MetAP). Some of these salicylate derivatives showed similar potency and metalloform selectivity, and some showed considerable antibacterial activity. These findings are consistent with our previous conclusion that Fe(II) is the likely metal used by MetAP in bacterial cells and provide new lead structures that can be further developed as novel antibacterial agents.
