@article{Wang_Zhao_Yin_Yuan_Wang_Wang_Wang_Ye_Chen_Guo_Xie_2018, title={In-vitro characterisation of a novel antimicrobial agent, TNP-2092, against Helicobacter pylori clinical isolates}, volume={148}, url={https://smw.ch/index.php/smw/article/view/2501}, DOI={10.4414/smw.2018.14630}, abstractNote={<p><strong>BACKGROUND AND OBJECTIVES</strong> <p>TNP-2092 is a novel dual-action lead compound consisting of rifamycin SV and 4H-4-oxo-quinolizine pharmacophores, with a broad spectrum of antibacterial activities. This compound is currently in the early stage of clinical development for <em>Helicobacter pylor</em>i infection. The aim of the present study was to determine the antibacterial activity of TNP-2092 against <em>H. pylori</em> isolated from primary patients.</p> <strong>METHODS</strong> <p>A total of 100 <em>H. pylori</em> clinical isolates from primary patients were selected. The minimum inhibitory concentrations (MICs) for clarithromycin, levofloxacin, rifampin and TNP-2092 were determined using an agar dilution method. A time-kill study was performed with different concentrations of TNP-2092 relevant to MIC against <em>H. pylori</em> ATCC strain 43504 for up to 24 hours. The time-kill study with drug concentrations of 0–4 × MIC was also used to determine the antibacterial activity of TNP-2092 against <em>H. pylori</em> under different pH conditions (pH 4–7).</p> <strong>RESULTS</strong> <p>The primary resistance percentages to clarithromycin, levofloxacin, rifampin and TNP-2092 were 13, 18, 1 and 1%, respectively. TNP-2092 killing kinetics were both concentration and time dependent. The effectiveness of TNP-2092 against <em>H. pylori</em> was gradually reduced with a decrease in pH.</p> <strong>CONCLUSIONS</strong> <p>TNP-2092 is highly active against <em>H. pylori</em> and against strains resistant to clarithromycin or levofloxacin. Its antibacterial activity is both concentration- and time-dependent .The antibacterial activity of TNP-2092 appears to be pH-dependent and is more active under neutral pH. TNP-2092 represents a promising new therapy for the treatment of <em>H. pylori</em> infection in primary patients.</p></p>}, number={2930}, journal={Swiss Medical Weekly}, author={Wang, Ben and Zhao, Qiaoyun and Yin, Wenzhu and Yuan, Ying and Wang, Xiaomei and Wang, You-hua and Wang, Hui and Ye, Wen and Chen, Shuping and Guo, Hai-long and Xie, Yong}, year={2018}, month={Jul.}, pages={w14630} }