Synthesis, structure and properties of N-aminosaccharin – A selective inhibitor of human carbonic anhydrase I. Issue 2 (11th January 2017) - Kuznetsov, Mikhail A.
Graphical abstract: Highlights: Previously unknown N -aminosaccharin was prepared. N -Aminosaccharin activity in different reactions has been investigated. N -Aminosaccharin was identified to be a selective low micromolar inhibitor of h CA I. Abstract: Previously unknown N -aminosaccharin was prepared in good yield via the one-step direct amination of saccharin sodium salt with hydroxylamine- O -mesitylenesulfonic acid (MSH) and its reactivity investigated. N -aminosaccharin and its derivatives were tested against h CA isoforms and the parent compound was identified to be a selective, low micromolar inhibitor (Ki = 8.8 μM) of h CA I. These findings provide a ligand-efficient starting point for the design of potent h CA I inhibitors – a promising drug target for retinal/cerebral edema treatment.