Further validation of strecker-type α-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

进一步验证 Strecker 型 α-氨基腈作为一类新型强效人类碳酸酐酶 II 抑制剂的有效性:使用差示扫描荧光法在公共领域内进行匹配扩展可实现化学型细化

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

Abstract

Testing of an expanded, 800-compound set of analogues of the earlier described Strecker-type α-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. [Formula: see text].

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