Carbonic anhydrase inhibitory properties of novel sulfonamide derivatives of aminoindanes and aminotetralins

AKBABA Y., AKINCIOGLU A., GOCER H., GÖKSU S., GÜLÇİN İ., Supuran C. T.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.29, sa.1, ss.35-42, 2014 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 29 Sayı: 1
  • Basım Tarihi: 2014
  • Doi Numarası: 10.3109/14756366.2012.750311
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.35-42
  • Anahtar Kelimeler: Aminoindane, aminotetralin, carbonic anhydrase, enzyme inhibition, sulfonamide, ERYTHROCYTE ISOZYMES I, PHENOLIC-COMPOUNDS, VITRO INHIBITION, ENZYME-ACTIVITY, VIVO, ACETAZOLAMIDE, PURIFICATION, DANTROLENE, MELATONIN, BINDING
  • Atatürk Üniversitesi Adresli: Evet

Özet

Six sulfonamides derived from indanes and tetralines were synthesized. The human carbonic anhydrase isozymes hCA I and hCA II inhibition effects of the synthesized sulfonamides were determined. From these compounds, while N-(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl) methane sulfonamide showed the most potent inhibitory effect against hCA I (K-i = 46 +/- 5.4 mu M, r(2) = 0.978), N-(1,2,3,4-tetrahydronaphthalene-2-yl) methanesulfonamide was found to have the best inhibitory effect against hCA II (K-i = 94 +/- 7.6 mu M, r(2) = 0.982).