Tetrahedron Letters, 2017, 58, 172–174

M.A. Kuznetsov, A.N. Shestakov, M. Zibinsky, M. Krasavin, C.T. Supuran, S. Kalinin, M. Tanç

“Synthesis, structure and properties of N-aminosaccharin – A selective inhibitor of human carbonic anhydrase I”

Tetrahedron Letters, 2017, 58, 172–174

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 hCA isoforms and the parent compound was identified to be a selective, low micromolar inhibitor (Ki = 8.8 lM) of hCA I. These findings provide a ligand-efficient starting point for the design of potent hCA I inhibitors – a promising drug target for retinal/cerebral edema treatment.


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