a Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Florence , Italy.
b Centre of Advanced Research in Bionanoconjugates and Biopolymers Department , " Petru Poni" Institute of Macromolecular Chemistry , Iasi , Romania.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):244-249. doi: 10.1080/14756366.2018.1547287.
A series of benzenesulfonamides incorporating selenazoles with diverse substitution patterns were investigated as inhibitors of six bacterial carbonic anhydrases (CAs, EC 4.2.1.1) from bacterial pathogens, such as Helicobacter pylori (hpCAα was the investigated enzyme), Vibrio cholerae (all the three CAs from this pathogen were considered, VchCAα, VchCAβ and VchCAγ) and Burkholderia pseudomallei (with its two CAs, BpsCAβ and BpsCAγ). All these sulfonamides were effective CA inhibitors, with potencies in the low micromolar or submicromolar range, making them attractive as lead compounds for designing antibacterials with a novel mechanism of action, which could counteract the extensive resistance problem observed with many clinically used antibiotics.
研究了一系列苯磺酰胺类化合物,其中包含具有不同取代模式的硒唑,作为来自细菌病原体的六种碳酸酐酶(CA,EC 4.2.1.1)的抑制剂,如幽门螺杆菌(hpCAα是研究的酶)、霍乱弧菌(来自该病原体的所有三种 CA,VchCAα、VchCAβ 和 VchCAγ)和类鼻疽伯克霍尔德菌(其两种 CA,BpsCAβ 和 BpsCAγ)。所有这些磺胺类药物都是有效的 CA 抑制剂,其效力在低微摩尔或亚微摩尔范围内,使它们成为设计具有新型作用机制的抗菌药物的有吸引力的先导化合物,可以对抗许多临床使用的抗生素广泛存在的耐药问题。