Sezione di Scienze Farmaceutiche, NEUROFARBA Dept., Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy.
Centre of Advanced Research in Bionanoconjugates and Biopolymers Department, "Petru Poni" Institute of Macromolecular Chemistry, 700487 Iasi, Romania.
Int J Mol Sci. 2020 Jan 17;21(2):598. doi: 10.3390/ijms21020598.
A series of 2-thio- and 2-seleno-acetamides bearing the benzenesulfonamide moiety were evaluated as Carbonic Anhydrase (CA, EC 4.2.1.1) inhibitors against different pathogenic bacteria such as the (VchCA-α and VchCA-β), (BpsCA-β and BpsCA-γ), (Rv3723-β) and the (StCA2-β). The molecules represent interesting leads worth developing as innovative antibacterial agents since they possess new mechanism of action and isoform selectivity preferentially against the bacterial expressed CAs. The identification of potent and selective inhibitors of bacterial CAs may lead to tools also useful for deciphering the physiological role(s) of such proteins.
一系列含有苯磺酰胺部分的 2-硫代和 2-硒代乙酰胺被评估为碳酸酐酶(CA,EC 4.2.1.1)抑制剂,针对不同的致病细菌,如 (VchCA-α 和 VchCA-β)、 (BpsCA-β 和 BpsCA-γ)、 (Rv3723-β)和 (StCA2-β)。这些分子代表了值得开发的有前途的先导化合物,因为它们具有新的作用机制和同工酶选择性,优先针对细菌表达的 CA。鉴定出强效和选择性的细菌 CA 抑制剂可能会产生对这些蛋白质的生理作用进行解码也有用的工具。