Further validation of strecker-type alpha-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scanning fluorimetry leads to chemotype refinement

Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasia Griniukova, Petro Borysko, Andrea Angeli, Claudiu T. Supuran

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    Abstract

    Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type alpha-aminonitriles (selected from publicly available Enamine Ltd. Screening Collection) in thermal shift assay against bovine carbonic anhydrase (bCA) led to further validation of this new class of inhibitors and identification a new, refined chemotype represented by inhibitors with 10-improved potency.


    Original languageEnglish
    Pages (from-to)165-171
    JournalJournal of Enzyme Inhibition and Medicinal Chemistry
    Volume35
    Issue number1
    Early online date22 Nov 2019
    DOIs
    Publication statusPublished - 2020

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