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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >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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Carbonic anhydrase inhibitors. Phenols incorporating 2- or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase

机译：碳酸酐酶抑制剂。含有2-或3-吡啶基-乙烯基羰基和叔胺基团的酚强烈抑制啤酒酵母β-碳酸酐酶

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摘要

A series of phenols incorporating tertiary amine and trans-pyridylethenyl-carbonyl moieties were assayed as inhibitors of the β-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 KIs 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 KIs in the range of 0.78–23.5?μM (hCA I) and 10.8–52.4?μM (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.
机译：测定了一系列掺入叔胺和反式吡啶基乙烯基-羰基部分的酚，作为啤酒酵母（Saccharomyces cerevisiae，ScCA）的β-碳酸酐酶（CA，EC 4.2.1.1）的抑制剂。这些化合物中的一种是低纳摩尔浓度的ScCA抑制剂，而其余的则以23.5–95.4？nM的K I s抑制酶。脱靶人（h）同工型hCA I和hCA II受这些酚的抑制作用要小得多，K I s在0.78–23.5？μM（hCA I）和10.8–52.4之间？μM（hCA II）。与经典的唑类药物相比，模型生物酿酒酵母和这种特定的酶可能对检测具有新型作用机制的抗真菌药物有用，而传统的唑类药物对它们产生了明显的耐药性。

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