Angeli Andrea, Abbas Ghulam, Del Prete Sonia, Carta Fabrizio, Capasso Clemente, Supuran Claudiu T
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. 2017 Dec;75:170-172. doi: 10.1016/j.bioorg.2017.09.016. Epub 2017 Sep 21.
A series of acyl selenoureido benzensulfonamides was evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against two Vibrio cholerae such enzymes (VchCAα over VchCAβ) belonging to the α- and β-classes, potential novel targets for anti-infective drugs development. These compounds showed strong inhibitory action against VchCAα over VchCAβ and excellent selectivity over the human (h) off-target isoforms hCA I and II. Identification of potent and possibly selective inhibitors of VchCAα and/or VchCAβ over the human counterparts may lead to pharmacological tools useful for understanding the physiological role(s) of these under-investigated proteins, possibly involved in the virulence of the bacterium and colonization of the host in bicarbonate rich regions of the gastro-intestinal tract.
一系列酰基硒脲基苯磺酰胺被评估作为碳酸酐酶（CA，EC 4.2.1.1）抑制剂，用于对抗两种霍乱弧菌的此类酶（VchCAα优于VchCAβ），它们分别属于α-和β-类，是抗感染药物开发的潜在新靶点。这些化合物对VchCAα的抑制作用强于VchCAβ，并且对人（h）脱靶同工型hCA I和II具有出色的选择性。鉴定出对VchCAα和/或VchCAβ具有强抑制作用且相对于人类对应物具有选择性的抑制剂，可能会产生有助于理解这些研究不足的蛋白质生理作用的药理学工具，这些蛋白质可能参与细菌的毒力以及在胃肠道富含碳酸氢盐区域中宿主的定殖。
