首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >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
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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

机译:进一步验证STLecter型α-氨基腈作为新类有效的人类碳酸酐酶II抑制剂:使用差示扫描荧光测定致趋化性细化,在公共领域中击中膨胀

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摘要

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].
机译:测试较早描述的膨胀型α-氨基腈(选自可公开的Enamine Ltd.筛选收集)的膨胀的800化合物的类似物的试验,用于对牛碳酸酐酶(BCA)的热移位测定导致对此新的进一步验证抑制剂类和鉴定抑制剂的新的精制趋化型,其具有10改善的效力。 [公式:见文字]。

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