Mechanochemical synthesis and in vitro anti-Helicobacter pylori and uresase inhibitory activities of novel zinc(II)-famotidine complex

被引：33

作者：

Amin, Muhammad ^{[2
,3
]}

Iqbal, Mohammad S. ^{[1
]}

Hughes, Roy W. ^{[3
]}

Khan, Safyan A. ^{[3
]}

Reynolds, Paul A. ^{[3
]}

Enne, Virve I. ^{[4
]}

Sajjad-ur-Rahman ^{[5
]}

Mirza, Akmal S. ^{[6
]}

机构：

[1] Govt Coll Univ, Dept Chem, Lahore 54000, Pakistan

[2] Univ Sargodha, Dept Chem, Sargodha, Pakistan

[3] Univ Bristol, Sch Chem, Bristol, Avon, England

[4] Univ Bristol, Sch Med Sci, Dept Cellular & Mol Med, Bristol BS8 1TD, Avon, England

[5] Univ Agr Faisalabad, Dept Microbiol, Faisalabad, Pakistan

[6] Punjab Med Coll, Dept Med, Faisalabad, Pakistan

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2010年 / 25卷 / 03期

关键词：

Zinc complexes; zinc-famotidine; antiulcer drugs; metal-based drugs; anti-H. pylori activity; mechanochemical synthesis; urease inhibition; UREASE INHIBITORS; ZINC; SUSCEPTIBILITY; ANALOGS; ACID;

D O I：

10.3109/14756360903179518

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：

The mechanochemical synthesis and characterization of a zinc complex with famotidine is described. The complex was characterized by microanalysis and a number of spectroscopic techniques. The complex was of M:L dihydrate type. Derivatization of famotidine with zinc appears to enhance the activity of the drug by inhibiting the growth of Helicobacter pylori (two reference and 34 clinical isolates). The complex inhibited the growth of H. pylori in an MIC range of 1-8 mu g mL<SU-1</SU. The anti-H. pylori activity of the zinc-famotidine complex against antibiotic-resistant strains was nearly comparable to that of antibiotic-susceptible strains. The complex was found to be far less toxic than the parent drug, as demonstrated by its higher LD50 value. In the human urease enzyme inhibition assay the complex exhibited significant inhibition. The new complex appears to be more useful in eradicating both the antibiotic-susceptible and antibiotic-resistant strains of H. pylori.</.

引用

页码：383 / 390

页数：8

共 34 条

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Syntheses, Urease Inhibition, and Antimicrobial Studies of Some Chiral 3-Substituted-4-amino-5-thioxo-1H,4H-1,2,4-triazoles [J].