A series of polyphenolic derivatives, including resveratrol, dobutamine, curcumin, catechin and silymarine were investigated for the inhibition of all the catalytically active mammalian isozymes of the metalloprotein carbonic anhydrase (CA, EC 4.2.1.1), that is, CA I-CA XV. These polyphenols effectively inhibited CAs, with K(I)s in the range of 380 nM-12.02 microM. The various isozymes showed quite diverse inhibition profiles with these compounds, which possess scaffolds not present in other investigated CA inhibitors (CAIs). These data may lead to drug design campaigns of effective CAIs possessing a diverse inhibition mechanism compared to sulfonamide/sulfamate inhibitors, based on such less investigated scaffolds.
Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV / A. Innocenti;I. Gülçin;A. Scozzafava;C. T. Supuran. - In: BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS. - ISSN 1464-3405. - STAMPA. - 20:(2010), pp. 5050-5053. [10.1016/j.bmcl.2010.07.038]
Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV.
SCOZZAFAVA, ANDREA;SUPURAN, CLAUDIU TRANDAFIR
2010
Abstract
A series of polyphenolic derivatives, including resveratrol, dobutamine, curcumin, catechin and silymarine were investigated for the inhibition of all the catalytically active mammalian isozymes of the metalloprotein carbonic anhydrase (CA, EC 4.2.1.1), that is, CA I-CA XV. These polyphenols effectively inhibited CAs, with K(I)s in the range of 380 nM-12.02 microM. The various isozymes showed quite diverse inhibition profiles with these compounds, which possess scaffolds not present in other investigated CA inhibitors (CAIs). These data may lead to drug design campaigns of effective CAIs possessing a diverse inhibition mechanism compared to sulfonamide/sulfamate inhibitors, based on such less investigated scaffolds.
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