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Antibiotics are currently used for the treatment of <i>Helicobacter pylori</i> (<i>H. pylori</i>), which is confirmed to be the major cause of gastric disorders. However, the long-term consumption of antibiotics has already caused antibiotic resistance and side effects in vivo. Therefore, there is an emerging need for searching for safe and effective anti-<i>H. pylori</i> agents. Inspired by the excellent bioactivities of cinnamic acid, a series of cinnamic acid derivatives (compounds <b>1</b>–<b>30</b>) were synthesized and determined for <i>H. pylori</i> inhibition. The initial screening revealed that compound <b>23</b>, a 2,4-dinitro cinnamic acid derivative containing 4-methoxyphenol, showed excellent <i>H. pylori</i> inhibition with an MIC value of 4 μM. Further studies indicated that compound <b>23</b> showed anti-bacterial activity and had a bactericidal effect on <i>H. pylori</i> due to the destruction of the bacterial structure. Molecular docking analysis revealed that the 2,4-dinitro groups in cinnamic acid moiety formed hydrogen bonding with amino acid residues in an active pocket of <i>H. pylori</i> protein. Interestingly, the ester moiety fitted into the hydrophobic pocket, attaining additional stability to compound <b>23</b>. Above all, the present study reveals that compound <b>23</b> could be considered a promising anti-<i>H. pylori</i> agent to treat <i>H. pylori</i> causing gastritis.