Sulfapyridine-like benzenesulfonamide derivatives as inhibitors of carbonic anhydrase isoenzymes I, II and VI.

ALP C., OZSOY S., ALP N. A., ERDEM D., GÜLTEKİN M. S., KÜFREVİOĞLU Ö. İ., ...Daha Fazla

Journal of enzyme inhibition and medicinal chemistry, cilt.27, sa.6, ss.818-24, 2012 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 27 Sayı: 6
  • Basım Tarihi: 2012
  • Doi Numarası: 10.3109/14756366.2011.617745
  • Dergi Adı: Journal of enzyme inhibition and medicinal chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.818-24
  • Anahtar Kelimeler: Carbonic anhydrase, inhibition, benzenesulfonamides, ISOZYME-II, THERAPEUTIC APPLICATIONS, RAINBOW-TROUT, HUMAN SERUM, PURIFICATION, SULFONAMIDES, ENZYMES, BINDING, DESIGN, SERIES
  • Atatürk Üniversitesi Adresli: Evet

Özet

The inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I, II and human serum isozyme VI, with a series of tosylited aromatic amine derivatives was investigated. The K-I ranges of compounds 1-14 and acetazolamide against hCA I ranged between 1.130 and- 448.2 mu M, against hCA II between 0.103 and- 14.3 mu M, and against hCA VI ranged between 0.340 and- 42.39 mu M. Tosylited aromatic amine derivatives are thus interesting hCA I, II and VI inhibitors, and might be used as leads for generating enzyme inhibitors eventually targeting other isoforms which have not been assayed yet for their interactions with such agents.