Synthesis and evaluation of N-heteroarylsubstituted triazolosulfonamides as carbonic anhydrase inhibitors

Balci A., Arslan M., NIXHA A. R., Bilen C., Ergun A., Gencer N.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.30, sa.3, ss.377-382, 2015 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 30 Sayı: 3
  • Basım Tarihi: 2015
  • Doi Numarası: 10.3109/14756366.2014.940933
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.377-382
  • Anahtar Kelimeler: Carbonic anhydrase, enzyme inhibitor, sulfonamide, triazole, IN-VITRO INHIBITION, ISOFORMS I, SULFONAMIDE INHIBITORS, ANTIFUNGAL AGENTS, DERIVATIVES, 1,2,4-TRIAZOLE, COUMARINS, ENZYME
  • Yıldız Teknik Üniversitesi Adresli: Hayır

Özet

A new series of N-heteroarylsubstituted triazolosulfonamide compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA) I and II were evaluated. Compounds (3 a-k) were prepared by propargylation of N-heteroaryl compounds. Compound 5 was obtained from sulfanilamide and sodium nitrite followed by addition of sodium azide. The products (6 a-k) were synthesized from compounds 3 and 5. The results showed that all the synthesized compounds were inhibited the CA isoenzymes activity. Figure 6a (IC50 = 0.52 mu M for hCA I and 0.34 mu M for hCA II) has the most inhibitory effect among the synthesized compounds.