Riafrecha Leonardo E, Vullo Daniela, Ouahrani-Bettache Safia, Köhler Stephan, Dumy Pascal, Winum Jean-Yves, Supuran Claudiu T, Colinas Pedro A
a LADECOR, Departamento de Química, Facultad de Ciencias Exactas , Universidad Nacional de La Plata , La Plata , Argentina .
b Laboratorio di Chimica Bioinorganica , Universitá degli Studi di Firenze , Sesto Fiorentino (Firenze) , Italy .
J Enzyme Inhib Med Chem. 2015 Dec;30(6):1017-20. doi: 10.3109/14756366.2014.986120. Epub 2015 Feb 13.
A small series of C-glycosides containing the phenol moiety was tested for the inhibition of the β-class carbonic anhydrases (βCAs, EC 4.2.1.1) from Brucella suis. Many compounds showed activities in the micromolar or submicromolar range and excellent selectivity for pathogen CAs over human isozymes. Glycosides incorporating the 3-hydroxyphenyl moiety showed the best inhibition profile, and therefore this functionality represents lead for the development of novel anti-infectives with a new mechanism of action.
对一系列含有酚部分的C-糖苷进行了测试，以检测其对猪布鲁氏菌β-类碳酸酐酶（βCAs，EC 4.2.1.1）的抑制作用。许多化合物表现出微摩尔或亚微摩尔范围内的活性，并且对病原体碳酸酐酶相对于人同工酶具有优异的选择性。含有3-羟基苯基部分的糖苷表现出最佳的抑制谱，因此该官能团代表了开发具有新作用机制的新型抗感染药物的先导物。
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