Chromone containing sulfonamides as potent carbonic anhydrase inhibitors

EKİNCİ D., al-Rashida M., Abbas G., ŞENTÜRK M., Supuran C. T.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.27, sa.5, ss.744-747, 2012 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 27 Sayı: 5
  • Basım Tarihi: 2012
  • Doi Numarası: 10.3109/14756366.2011.614607
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.744-747
  • Anahtar Kelimeler: Human carbonic anhydrase, enzyme inhibitors, sulfonamides, schiff's base, IN-VITRO INHIBITION, THERAPEUTIC APPLICATIONS, PHENOLIC-COMPOUNDS, ISOZYME-II, X-RAY, BINDING, AGENTS, ACTIVATORS
  • Ondokuz Mayıs Üniversitesi Adresli: Evet

Özet

A series of sulfonamide derivatives incorporating substituted 3-formylchromone moieties were investigated for the inhibition of three human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, hCA I, II, and VI. All these compounds, together with the clinically used sulfonamide acetazolamide, were investigated as inhibitors of the physiologically relevant isozymes I, II (cytosolic), and VI (secreted isoform). These sulfonamides showed effective inhibition against all these isoforms with K's in the range of 0.228 to 118 mu M. Such molecules can be used as leads for discovery of novel effective CA inhibitors against other isoforms with medicinal chemistry applications.