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

Sinan Bilginer, Elif Unluer, Halise İnci Gül, Ebru Mete, Semra Isık, Daniela Vullo, Ozen Ozensoy-Guler, Serap Beyaztas, Clemente Capasso, Claudiu T. Supuran

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY Cilt 29 · Sayı 4 · ss. 495–499 · 01.08.2014
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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.

Anahtar kelimeler

benzenesulfonamides Antifungalscarbonic anhydrase phenols pyridylethenyl-carbonyl Saccharomyces cerevisiae CLASS ENZYME CANDIDA-GLABRATA SULFONAMIDES

Atıf için künye

Bilginer, S., Unluer, E., Gül, H. İ., Mete, E., Isık, S., Vullo, D., Ozensoy-Guler, O., Beyaztas, S., Capasso, C., & Supuran, C. T. (2014). Carbonic anhydrase inhibitors. Phenols incorporating 2-or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae beta-carbonic anhydrase. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 29(4), 495–499. https://doi.org/10.3109/14756366.2013.806497

BibTeX 
@article{bilginer2014-19857,
  author = {Bilginer, Sinan and Unluer, Elif and Gül, Halise İnci and Mete, Ebru and Isık, Semra and Vullo, Daniela and Ozensoy-Guler, Ozen and Beyaztas, Serap and Capasso, Clemente and Supuran, Claudiu T.},
  title = {Carbonic anhydrase inhibitors. Phenols incorporating 2-or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae beta-carbonic anhydrase},
  journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
  year = {2014},
  volume = {29},
  number = {4},
  pages = {495--499},
  issn = {1475-6366},
  doi = {10.3109/14756366.2013.806497},
  url = {https://akademik.atauni.edu.tr/yayinlar/19857-carbonic-anhydrase-inhibitors-phenols-incorporating-2-or-3-pyridyl}
}