Synthesis of some natural sulphonamide derivatives as carbonic anhydrase inhibitors


Gokcen T., Al M., Topal M., GÜLÇİN İ., Ozturk T., Goren A. C.

ORGANIC COMMUNICATIONS, cilt.10, sa.1, ss.15-23, 2017 (ESCI) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 10 Sayı: 1
  • Basım Tarihi: 2017
  • Doi Numarası: 10.25135/acg.oc.4.16.05.418
  • Dergi Adı: ORGANIC COMMUNICATIONS
  • Derginin Tarandığı İndeksler: Emerging Sources Citation Index (ESCI), Scopus
  • Sayfa Sayıları: ss.15-23
  • İstanbul Teknik Üniversitesi Adresli: Evet

Özet

Carbonic anhydrase inhibitor; sulphonamides; p-hydroxybenzoic acid; 3,4,5-trihydroxybenzoic acid (gallic acid).Carbonic anhydrase inhibitors are both in clinical use as antiglaucoma, diuretics, antiepileptics and management of altitude sickness, and under investigation as anticancer, anticonvulsant and antiobesity agents. Sulphonamides have been known for decades as carbonic anhydrase inhibitors and are in clinical use. Sulphonamide derivatives of p-hydroxybenzoic acid and 3,4,5-trihydroxybenzoic acid (gallic acid) were synthesized and their inhibition values over hCA I and hCA II isozymes, purified from human erythrocyte cells by Sepharose-4B-L-tyrosine-sulphanilamide, were determined. Compounds synthesized showed efficient carbonic anhydrase inhibition activity at low nM levels.