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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

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journal contribution
posted on 2019-11-22, 08:10 authored by Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasia Griniukova, Petro Borysko, Andrea Angeli, Claudiu T. Supuran

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.

Funding

This research was supported by the Russian Federation Government Megagrant 14.W03.031.0025.

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