Carbonic anhydrase inhibitors. Phenols incorporating 2- or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase. (August 2014)

• Record Type: Journal Article
• Authors: Bilginer, Sinan; Unluer, Elif; Gul, Halise Inci; Mete, Ebru; Isik, Semra; Vullo, Daniela; Ozensoy-Guler, Ozen; Beyaztas, Serap; Capasso, Clemente; Supuran, Claudiu T.
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 29:Number 4(2014:Aug.)
• Page Start: 495
• Page End: 499
• Publication Date: 2014-08
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2013.806497
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title>Abstract</title> <p>A series of phenols incorporating tertiary amine and <italic>trans</italic>-pyridylethenyl-carbonyl moieties were assayed as inhibitors of the β-carbonic anhydrase (CA, EC 4.2.1.1) from <italic>Saccharomyces cerevisiae</italic>, ScCA. One of these compounds was a low nanomolar ScCA inhibitor, whereas the remaining ones inhibited the enzyme with K_Is 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_Is in the range of 0.78–23.5 µM (hCA I) and 10.8–52.4 µM (hCA II). The model organism <italic>S. cerevisiae</italic> 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.</p> </abstract>