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Published on: June 13, 2025
Developing potential Helicobacter pylori urease inhibitors from novel oxoindoline derivatives: Synthesis, biological
Yu-Shun Yang1, Mi-Mi Su1, Xu-Ping Zhang1
1State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210023, China.
Abstract:
By recruiting the important moiety from Shikonin, a series of novel oxoindoline derivatives S1-S20 have been synthesized for inhibiting H. pylori urease. The most potent compound S18 displayed better activity (IC50 = 0.71 μM; MIC = 0.48 μM) than the positive controls AHA (IC50 = 17.2 μM) and Metronidazole (MIC = 31.3 μM). With low cytotoxicity, it showed considerable potential for further development. Docking simulation revealed the possible binding pattern of this series. 3D QSAR model was built to discuss SAR and give useful hints for future modification.
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