Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy.
Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy; Department of Biological Sciences and Chemistry, University of Nizwa, Birkat Al-Mauz, P.O. Box 33, Nizwa 616, Oman.
Bioorg Chem. 2018 Sep;79:319-322. doi: 10.1016/j.bioorg.2018.05.015. Epub 2018 May 18.
A series of selenides bearing benzenesulfonamide moieties was evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against the pathogenic bacteria Vibrio cholerae (VchCAα and VchCAβ) and Burkholderia pseudomallei (BpsCAβ) enzymes. The molecules represent an interesting lead for antibacterial agents with a possibly new mechanism of action showing excellent inhibitory action and selectivity for inhibiting VchCAα and BpsCAβ over the human (h) off-target isoforms hCA I and II. Identification of potent and possibly selective inhibitors of bacteria CAs over the human counterparts may lead to pharmacological tools useful for understanding the physiological role(s) of these under-investigated proteins.
一系列含有苯磺酰胺基团的硒化物被评估为碳酸酐酶（CA，EC 4.2.1.1）抑制剂，用于抑制致病细菌霍乱弧菌（VchCAα 和 VchCAβ）和类鼻疽伯克霍尔德菌（BpsCAβ）。这些分子代表了具有可能新作用机制的抗菌药物的一个有趣的先导物，对抑制 VchCAα 和 BpsCAβ 具有优异的抑制作用和选择性，而对人（h）靶标同工酶 hCA I 和 II 则没有作用。鉴定出对人类同工酶具有强大且可能选择性的细菌 CA 抑制剂，可能会产生有用的药理学工具，有助于理解这些研究不足的蛋白质的生理作用。
