C -glycosides incorporating the 6-methoxy-2-naphthyl moiety are selective inhibitors of fungal and bacterial carbonic anhydrases

Leonardo E. Riafrecha; Daniela Vullo; Claudiu T. Supuran; Pedro A. Colinas

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C -glycosides incorporating the 6-methoxy-2-naphthyl moiety are selective inhibitors of fungal and bacterial carbonic anhydrases

机译：掺入6-甲氧基-2-萘基的C-糖苷是真菌和细菌碳酸酐酶的选择性抑制剂

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A small series of C-glycosides containing the methoxyaryl moieties was tested for the inhibition of the β-class carbonic anhydrases (CAs, EC 4.2.1.1) from Cryptococcus neoformans and Brucella suis. Many compounds showed activities in the micromolar or submicromolar range and excellent selectivity for pathogen CAs over human isozymes. The deprotected glycosides incorporating the 6-methoxy-2-naphthyl moiety showed the best inhibition profile and therefore represent leads for the development of novel anti-infectives with a new mechanism of action.

机译：测试了一系列含有甲氧基芳基部分的C-糖苷对新隐球菌和猪布鲁氏菌的β类碳酸酐酶（CAs，EC 4.2.1.1）的抑制作用。许多化合物显示出在微摩尔或亚微摩尔范围内的活性，并且对病原体CA的选择性优于人类同工酶。结合有6-甲氧基-2-萘基部分的去保护的糖苷显示出最佳的抑制特性，因此代表了开发具有新作用机制的新型抗感染药的线索。

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《Journal of enzyme inhibition and medicinal chemistry.》 |2015年第5期|共5页
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Leonardo E. Riafrecha; Daniela Vullo; Claudiu T. Supuran; Pedro A. Colinas;
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1. C-glycosides incorporating the 6-methoxy-2-naphthyl moiety are selective inhibitors of fungal and bacterial carbonic anhydrases [J] . Riafrecha Leonardo E., Vullo Daniela, Supuran Claudiu T., Journal of enzyme inhibition and medicinal chemistry. . 2015,第1a6期

机译：掺入6-甲氧基-2-萘基的C-糖苷是真菌和细菌碳酸酐酶的选择性抑制剂
2. Inhibition studies of bacterial, fungal and protozoan beta-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties [J] . Ceruso Mariangela, Carta Fabrizio, Osman Sameh M., Bioorganic and medicinal chemistry . 2015,第15期

机译：带有磺酰胺基团的席夫碱对细菌，真菌和原生动物β-类碳酸酐酶的抑制研究
3. Carbonic anhydrase inhibitors. Phenols incorporating 2-or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae beta-carbonic anhydrase [J] . Bilginer Sinan, Unluer Elif, Gul Halise Inci, Journal of enzyme inhibition and medicinal chemistry. . 2014,第1a6期

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
4. STABILITY STUDY IN PLASMA OF NOVEL ESTER-LINKED NSAID - CARBONIC ANHYDRASE INHIBITOR HYBRIDS [C] . Silvia Bua, Marta Menicatti, Paola Gratteri, International Mass Spectrometry Conference . 2018

机译：新型酯连接NSAID - 碳酸酐酶抑制剂杂交种血浆稳定性研究
5. High-throughput screening studies of inhibition of human carbonic anhydrase II and bacterial flagella antimicrobial activity. [D] . Barrese, Albert A., III. 2010

机译：高通量筛选研究抑制人类碳酸酐酶II和细菌鞭毛的抗菌活性。
6. Inhibition of bacterial α- β- and γ-class carbonic anhydrases with selenazoles incorporating benzenesulfonamide moieties [O] . Andrea Angeli, Mariana Pinteala, Stelian S. Maier, 2019

机译：掺有苯磺酰胺部分的亚硒唑对细菌α-β-和γ-类碳酸酐酶的抑制作用
7. Carbonic anhydrase inhibitors. Phenols incorporating 2- or 3-pyridyl-ethenylcarbonyl and tertiary amine moieties strongly inhibit Saccharomyces cerevisiae β-carbonic anhydrase [O] . Sinan Bilginer, Elif Unluer, Halise Inci Gul, 2013

机译：碳酸酐酶抑制剂。掺入2-或3-吡啶基 - 乙基羰基和叔胺部分的酚强烈抑制酿酒酵母β-碳酸酐酶

C -glycosides incorporating the 6-methoxy-2-naphthyl moiety are selective inhibitors of fungal and bacterial carbonic anhydrases

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