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Selenides bearing benzenesulfonamide show potent inhibition activity against carbonic anhydrases from pathogenic bacteria Vibrio cholerae and Burkholderia pseudomallei
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2018-05-18 , DOI: 10.1016/j.bioorg.2018.05.015
Andrea Angeli 1 , Ghulam Abbas 2 , Sonia Del Prete 3 , Clemente Capasso 3 , Claudiu T Supuran 1
Affiliation  

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.



中文翻译:


带有苯磺酰胺的硒化物对霍乱弧菌和类鼻疽伯克霍尔德氏菌的碳酸酐酶具有有效的抑制活性



一系列带有苯磺酰胺部分的硒化物作为碳酸酐酶(CA,EC 4.2.1.1)抑制剂对致病菌霍乱弧菌(VchCAα和VchCAβ)和类鼻疽伯克霍尔德杆菌(BpsCAβ)酶进行了评估。这些分子代表了抗菌剂的一个有趣的先导,其可能具有新的作用机制,显示出与人 (h) 脱靶亚型 hCA I 和 II 相比,对 VchCAα 和 BpsCAβ 的优异抑制作用和选择性。鉴定出比人类对应物更有效且可能具有选择性的细菌 CA 抑制剂可能会产生有助于了解这些正在研究的蛋白质的生理作用的药理学工具。

更新日期:2018-05-18
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