Synthesis,structure and properties of N-aminosaccharin – A selective inhibitor of human carbonic anhydrase I |
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Authors: | Mikhail A Kuznetsov Aleksandr N Shestakov Mikhail Zibinsky Mikhail Krasavin Claudiu T Supuran Stanislav Kalinin Muhammet Tanç |
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Institution: | 1. Institute of Chemistry, Saint Petersburg State University, Universitetsky pr. 26, 198504 Saint Petersburg, Russia;2. Neurofarba Department, Universita degli Studi di Firenze, Florence, Italy |
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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 (Ki = 8.8 μM) 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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Keywords: | Oxidative aminoaziridination Ligand efficiency |
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