Accéder au contenu
Merck
  • 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.

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 (2019-11-23)
Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasia Griniukova, Petro Borysko, Andrea Angeli, Claudiu T Supuran
RÉSUMÉ

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].

MATÉRIAUX
Référence du produit
Marque
Description du produit

Sigma-Aldrich
Anhydrase carbonique from bovine erythrocytes, lyophilized powder, ≥2,000 W-A units/mg protein