Carbonic anhydrase inhibitors. Phenols incorporating 2- or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase.


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BİLGİNER S., Unluer E., GÜL H. İ. , METE E., Isik S., Vullo D., ...Daha Fazla

Journal of enzyme inhibition and medicinal chemistry, cilt.29, ss.495-9, 2014 (SCI Expanded İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 29 Konu: 4
  • Basım Tarihi: 2014
  • Doi Numarası: 10.3109/14756366.2013.806497
  • Dergi Adı: Journal of enzyme inhibition and medicinal chemistry
  • Sayfa Sayıları: ss.495-9

Özet

A series of phenols incorporating tertiary amine and trans-pyridylethenyl-carbonyl moieties were assayed as inhibitors of the beta-carbonic anhydrase (CA, EC 4.2.1.1) from Saccharomyces cerevisiae, ScCA. One of these compounds was a low nanomolar ScCA inhibitor, whereas the remaining ones inhibited the enzyme with K(I)s in the range of 23.5-95.4 nM. The off-target human (h) isoforms hCA I and hCA II were much less inhibited by these phenols, with K(I)s in the range of 0.78-23.5 mu M (hCA I) and 10.8-52.4 mu M (hCA II). The model organism S. cerevisiae and this particular enzyme may be useful for detecting antifungals with a novel mechanism of action compared to the classical azole drugs to which significant drug resistance emerged.