Spirobisnaphthalenes effectively inhibit carbonic anhydrase

Gocer H., Aslan A., GÜLÇİN İ., SUPURAN C. T.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.31, sa.3, ss.503-507, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 31 Sayı: 3
  • Basım Tarihi: 2016
  • Doi Numarası: 10.3109/14756366.2015.1043298
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.503-507
  • Anahtar Kelimeler: Carbonic anhydrase, enzyme inhibition, enzyme purification, spirobisnaphthalenes, TROUT ONCORHYNCHUS-MYKISS, ERYTHROCYTES IN-VITRO, THERAPEUTIC APPLICATIONS, CLADOSPIRONE BISEPOXIDE, ABSOLUTE-CONFIGURATION, FUNGAL METABOLITES, ISOENZYMES I, DERIVATIVES, DEOXYPREUSSOMERINS, MELATONIN
  • Atatürk Üniversitesi Adresli: Evet

Özet

This study explores the correlation between human carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and II (hCA I, II) and the inhibitory features of some spirobisnaphthalene derivatives. A group of spirobisnaphthalenes was synthesized and their hCA I and II inhibitory effects was investigated. The K-i values were similar for both CA isoenzymes, the compounds showing good inhibitory activity. K-i values ranged between 1.60 and 460.42 mu M for hCA I and between 0.39 and 419.42 mu M for hCA II, respectively. The spirobisnaphthalenes derivatives might be useful for designing CA inhibitors belonging to novel chemotypes compared to the highly investigated sulfonamides, sulfamates or coumarins.