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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.
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页码:1035 / 1038
页数:7
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