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Metronidazole–Flavonoid Derivatives as Anti‐ Helicobacter pylori Agents with Potent Inhibitory Activity against HPE‐Induced Interleukin‐8 Production by AGS Cells
Author(s) -
Li HuanQiu,
Xu Chen,
Li HongSen,
Xiao ZhuPing,
Shi Lei,
Zhu HaiLiang
Publication year - 2007
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200700097
Subject(s) - bacillus subtilis , flavonoid , chemistry , antimicrobial , microbiology and biotechnology , helicobacter pylori , genistein , minimum inhibitory concentration , metronidazole , pharmacology , bacteria , biochemistry , antibiotics , biology , genetics , antioxidant , endocrinology
Three series of metronidazole–flavonoid derivatives were generated and evaluated for antimicrobial activity against H. pylori . Among these compounds, high anti‐ H. pylori activities were observed in isoflavones derivatives 4 – 7 , 19 , and 20 but exhibited no inhibitory activity against other sorts of bacteria and fungi, for example, Streptococcus pneumoniae, Bacillus subtilis, Escherichia coli, Pseudomonas fluorescence , and Aspergillus niger . Genistein derivative 6 with the potent activity (MIC=0.39 μg mL −1 ) was >50‐fold more than metronidazole, and comparable to the positive control amoxicillin. Additionally, compound 6 can significantly attenuate the increase in interleukin‐8 (IL‐8) levels in the AGS cells stimulated by H. pylori water extract (HPE) at concentrations of 15, 30, and 60 μmol L −1 , which did not show any effects on the cell viability.