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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

Authors :
Mikhail Krasavin
Stanislav Kalinin
Sergey Zozulya
Anastasia Griniukova
Petro Borysko
Andrea Angeli
Claudiu T. Supuran
Source :
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 165-171 (2020)
Publication Year :
2020
Publisher :
Taylor & Francis Group, 2020.

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.

Details

Language :
English
ISSN :
14756366 and 14756374
Volume :
35
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Journal of Enzyme Inhibition and Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
edsdoj.3b860d34fb7405fbc2cfb24b09d2294
Document Type :
article
Full Text :
https://doi.org/10.1080/14756366.2019.1693556