Synthesis and carbonic anhydrase inhibitory properties of novel chalcone substituted benzenesulfonamides
Bioorganic and Medicinal Chemistry Letters, cilt.26, sa.24, ss.5867-5870, 2016 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 26 Sayı: 24
- Basım Tarihi: 2016
- Doi Numarası: 10.1016/j.bmcl.2016.11.017
- Dergi Adı: Bioorganic and Medicinal Chemistry Letters
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.5867-5870
- Anahtar Kelimeler: Chalcone, Sulfonamides, Carbonic anhydrase, Inhibitors
- Sağlık Bilimleri Üniversitesi Adresli: Hayır
Özet
Carbonic anhydrases (CAs, EC 4.2.1.1) are crucial metalloenzymes involved in many bioprocesses, through catalysis of the reversible hydration/dehydration process of CO2/HCO3 −. The inhibition of human CA isoforms I and II with a new series of sulfonamide derivatives incorporating substituted chalcone moieties were studied in this study. All these newly synthesized sulfonamides demonstrated important inhibitory profiles to these CA isoforms with KIs in the range of 9.88 to 55.43 nM, making these compounds interesting leads, with potential applications in medicinal chemistry.