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 (K-1 = 8.8 mu M) 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. (C) 2016 Elsevier Ltd. All rights reserved.
Synthesis, structure and properties of N -aminosaccharin – A selective inhibitor of human carbonic anhydrase I / Mikhail A. Kuznetsov; Aleksandr N. Shestakov; Mikhail Zibinsky; Mikhail Krasavin; Claudiu T. Supuran; Stanislav Kalinin; Muhammet Tanç. - In: TETRAHEDRON LETTERS. - ISSN 0040-4039. - ELETTRONICO. - 58:(2017), pp. 0-0. [10.1016/j.tetlet.2016.12.005]
Synthesis, structure and properties of N -aminosaccharin – A selective inhibitor of human carbonic anhydrase I
Claudiu T. Supuran;
2017
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 hCA isoforms and the parent compound was identified to be a selective, low micromolar inhibitor (K-1 = 8.8 mu M) 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. (C) 2016 Elsevier Ltd. All rights reserved.
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