Accéder au contenu
Merck

Carbonic anhydrase inhibitors. Inhibition of cytosolic isoforms I, II, III, VII and XIII with less investigated inorganic anions.

Bioorganic & medicinal chemistry letters (2009-03-10)
Alessio Innocenti, Andrea Scozzafava, Claudiu T Supuran
RÉSUMÉ

An inhibition study of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isoforms I, II, III, VII and XIII with anions such as stannate(IV), selenate(VI), tellurate(VI), perosmate(VIII), persulfate, pyrophosphate(V), pyrovanadate(V), tetraborate, persulfate, perrhenate(VII), perrutenate(VII), selenocyanate, iminodisulfonate, fluorosulfate and trithiocarbonate is reported. Trithiocarbonate was the best inhibitor detected, showing affinities of 8.7-9.9 microM for CA I-III, of 36.15 mM for CA VII and of 0.43 mM for CA XIII. Considering trithiocarbonate as lead, we show that compounds incorporating the new zinc-binding group CS2-, such as among other the dithiocarbamates, are even more active inhibitors, with submicromolar inhibitory activity. New classes of CA inhibitors are being detected based on the CS2- zinc-binding group.

MATÉRIAUX
Référence du produit
Marque
Description du produit

Sigma-Aldrich
Sodium persulfate, reagent grade, ≥98%
Sigma-Aldrich
Sodium pyrophosphate tetrabasic, ≥95%
Sigma-Aldrich
Sodium selenate, ≥95% (elemental analysis)
Sigma-Aldrich
Sodium persulfate, purum p.a., ≥98% (RT)
Sigma-Aldrich
Sodium persulfate, BioUltra, ≥99%
Sigma-Aldrich
Sodium selenate, BioXtra
Sigma-Aldrich
Sodium persulfate, BioXtra, ≥99%