Synthesis and carbonic anhydrase inhibitory properties of 1,3-dicarbonyl derivatives of methylaminobenzene-sulfonamide

Demirci T., Arslan M., Bilen C., Demir D., Gencer N., Arslan O.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.29, sa.1, ss.132-136, 2014 (SCI-Expanded, Scopus)

Özet

1,3-Dicarbonyl derivatives of methylaminobenzene-sulfonamide were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and hCA II were evaluated. hCA I and hCA II from human erythrocytes were purified by a simple one-step procedure by using Sepharose 4B-L-tyrosine-sulfanilamide affinity column. Our results show that the synthesized compounds inhibited the activity of carbonic anhydrase (CA) I and CA II. Among them, 2b and 2e were found to be the most active (IC50 = 2.12 and 2.52 mu M) for hCA I and hCA II, respectively.