COMPOUNDS FOR THE TREATMENT OF DISEASES CAUSED BY OXALATE ACCUMULATION
申请人:UNIVERSIDAD DE GRANADA
公开号:US20200197418A1
公开(公告)日:2020-06-25
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 renal insufficiency (uremia or azotaemia) receiving haemodialysis or peritoneal dialysis, in particular patients treated with ascorbic acid (vitamin C), which is metabolised to oxalate, or patients with fibromyalgia and vulvar pain.
Salicylic Acid Derivatives Inhibit Oxalate Production in Mouse Hepatocytes with Primary Hyperoxaluria Type 1
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