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, ss.132-136, 2014 (SCI İndekslerine Giren Dergi)

  • Cilt numarası: 29 Konu: 1
  • Basım Tarihi: 2014
  • Doi Numarası: 10.3109/14756366.2012.757603
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Sayfa Sayısı: ss.132-136

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.