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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.
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2019-11-22 , DOI: 10.1080/14756366.2019.1693556
Mikhail Krasavin 1 , Stanislav Kalinin 1 , Sergey Zozulya 2, 3 , Anastasia Griniukova 2 , Petro Borysko 2 , Andrea Angeli 4 , Claudiu T Supuran 4
Affiliation  

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].

中文翻译:

strecker型α-氨基腈作为一类新型的有效人类碳酸酐酶II抑制剂得到了进一步的验证:使用差示扫描荧光法在公共领域内的命中扩展导致化学型的提高。

在针对牛碳酸酐酶(bCA)的热移分析中测试了先前描述的Strecker型α-氨基腈(选自公开的Enamine Ltd.筛选收藏)的扩展的800化合物类似物,从而进一步验证了这一新产品一类抑制剂并鉴定以抑制剂为代表的新的,完善的化学型,其效价提高了10。[公式:见文字]。
更新日期:2020-04-20
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