Sulfonamides with Potent Inhibitory Action and Selectivity against the α-Carbonic Anhydrase from Vibrio cholerae

被引：24

作者：

Ceruso, Mariangela ^{[1
]}

Del Prete, Sonia ^{[2
]}

Alothman, Zeid ^{[3
]}

Capasso, Clemente ^{[2
]}

Supuran, Claudiu T. ^{[1
,3
,4
]}

机构：

[1] Univ Florence, Lab Chim Bioinorgan, Dipartimento Chim, I-50019 Florence, Italy

[2] CNR, Ist Biosci & Biorisorse, I-80131 Naples, Italy

[3] King Saud Univ, Dept Chem, Coll Sci, Riyadh 11451, Saudi Arabia

[4] Univ Florence, Sect Pharmaceut & Nutriceut Sci, Neurofarba Dept, I-50019 Florence, Italy

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2014年 / 5卷 / 07期

关键词：

Carbonic anhydrase; enzyme inhibitor; sulfonamide; amino acid; Vibrio cholerae;

D O I：

10.1021/ml500192a

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

By using N-alpha-acetyl-L-lysine or GABA scaffolds and the conversion of the terminal amino group to the guanidine one, benzenesulfonamides incorporating water solubilizing moieties were synthesized. The new compounds were medium potency inhibitors of the cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isoforms I and II, and highly effective, nanomolar inhibitors of the pathogenic bacterial alpha-CA from Vibrio cholerae. These sulfonamides possess good selectivity for inhibiting the bacterial over the mammalian isoforms and may be used as tools to understand the role of bacterial CAs in pathogenesis.

引用

页码：826 / 830

页数：5

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