Synthesis and investigation of inhibition effects of new carbonic anhydrase inhibitors

ARSLAN O., Kufrevioglu O., NALBANTOGLU B.

BIOORGANIC & MEDICINAL CHEMISTRY, cilt.5, sa.3, ss.515-518, 1997 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 5 Sayı: 3
  • Basım Tarihi: 1997
  • Doi Numarası: 10.1016/s0968-0896(96)00272-6
  • Dergi Adı: BIOORGANIC & MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.515-518
  • Anahtar Kelimeler: carbonic anhydrase isozymes, carbonic anhydrase inhibitors, OCULAR PHARMACOLOGY, PRESSURE, BINDING, EYE, CO2
  • Atatürk Üniversitesi Adresli: Evet

Özet

Three new derivatives of 2-substituted 1,3,4-thiadiazole-5-sulfonamide have been synthesized. These compounds are 2-(3-chloropropionylamino)-1,3,4-thiadiazole-5-sulfonamide (1); 2-(2,2-dichloroacetylamino)-1,3,4-thiadiazole-5-sulfonamide (2); and 2-(3-phenylpropionylamino)-1,3,4-thiadiazole-5-sulfonamide (3). Inhibition effects of these compounds on carbonic anhydrase I and II have been investigated. By comparing I-50 and K-i values of the compounds, it has been found that compound 1 is a more potent inhibitor than acetazolamide (b) on carbonic anhydrase II. (C) 1997 Elsevier Science Ltd.