Acyl selenoureido benzensulfonamides show potent inhibitory activity against carbonic anhydrases from the pathogenic bacterium Vibrio cholerae

被引:25
作者
Angeli, Andrea [1 ]
Abbas, Ghulam [1 ,2 ]
Del Prete, Sonia [3 ]
Carta, Fabrizio [1 ]
Capasso, Clemente [3 ]
Supuran, Claudiu T. [1 ]
机构
[1] Univ Firenze, NEUROFARBA Dept, Sez Sci Farmaceut, Via Ugo Schiff 6, I-50019 Florence, Italy
[2] Univ Nizwa, Dept Biol Sci & Chem, POB 33, Nizwa 616, Oman
[3] CNR, Ist Biosci & Biorisorse, Via Pietro Castellino 111, I-80131 Naples, Italy
关键词
Carbonic anhydrase; Inhibitors; Metalloenzymes; Selenium; Acylseleno-ureido; Vibrio cholerae; ISOZYME-II; ALPHA; VII; IX; SULFONAMIDES; DISCOVERY; MOIETIES; ISOFORMS; TARGETS; DESIGN;
D O I
10.1016/j.bioorg.2017.09.016
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
摘要
A series of acyl selenoureido benzensulfonamides was evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against two Vibrio cholerae such enzymes (VchCA alpha over VchCA beta) belonging to the alpha- and beta-classes, potential novel targets for anti-infective drugs development. These compounds showed strong inhibitory action against VchCA alpha over VchCA beta and excellent selectivity over the human (h) off-target isoforms hCA I and II. Identification of potent and possibly selective inhibitors of VchCA alpha and/or VchCA beta 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. (C) 2017 Elsevier Inc. All rights reserved.
引用
收藏
页码:170 / 172
页数:3
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