Famotidine, an Antiulcer Agent, Strongly Inhibits Helicobacter pylori and Human Carbonic Anhydrases

被引：48
|
作者：
Angeli, Andrea [1 ]
Ferraroni, Marta [2 ]
Supuran, Claudiu T. [1 ]
机构：
[1] Univ Florence, NEUROFARBA Dept, Sez Sci Farmaceut, Via Ugo Schiff 6, I-50019 Florence, Italy
[2] Univ Florence, Dept Chem Ugo Schiff, Via Lastruccia 13, I-50019 Florence, Italy
来源：
ACS MEDICINAL CHEMISTRY LETTERS | 2018年 / 9卷 / 10期
关键词：
Carbonic anhydrase; famotidine; Helicobacter pylori; inhibitor; metalloenzymes; SULFONAMIDE INHIBITION; IN-VITRO; RANITIDINE; OMEPRAZOLE;
D O I：
10.1021/acsmedchemlett.8b00334
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Famotidine, an antiulcer drug incorporating a sulfamide motif, was investigated as carbonic anhydrase inhibitor (CAI). It acts as a nanomolar inhibitor of several human (hCA II, VI, VII and XII) and Helicobacter pylori CAs. The high resolution X-ray structures of famotidine bound to hCA I and II revealed interesting aspects related to its CA inhibition mechanism, offering the possibility to develop antibacterials with a novel mechanism of action.
引用
收藏
页码：1035 / 1038
页数：7
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