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

Demirci T., Arslan M., BİLEN Ç., DEMİR D., Gençer N., Arslan O.

Journal of Enzyme Inhibition and Medicinal Chemistry, cilt.29, sa.1, ss.132-136, 2014 (SCI-Expanded, Scopus) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 29 Sayı: 1
  • Basım Tarihi: 2014
  • Doi Numarası: 10.3109/14756366.2012.757603
  • Dergi Adı: Journal of Enzyme Inhibition and Medicinal Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.132-136
  • Anahtar Kelimeler: 1,3-dicarbonyl, Carbonic anhydrase, Enzyme inhibitor, Sulfonamide
  • Isparta Uygulamalı Bilimler Üniversitesi Adresli: Hayır

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 μM) for hCA I and hCA II, respectively. © 2014 Informa UK Ltd.