期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 11, 页码 5258-5264出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.08.045
关键词
Anti-Helicobacter pylori lead; Structural modification; SAR study
资金
- National Natural Science Foundation [30701044]
- Chinese Academy of Sciences [KSCX2-YW-R-117]
- National Science & Technology Major Project Key New Drug Creation and Manufacturing Program [2009ZX09301-001]
- Shanghai Municipal Scientific Foundation of the People's Republic of China [08JC1422300]
Psoralen (1a) was found to be a specific and potent antimicrobial lead against Helicobacter pylori (H. pylori) from a traditional Chinese medicine (TCM) in the bioassay directed isolation. A series of structurally diverse analogues of la were thus designed and synthesized to improve the antimicrobial potency, some of which showed more potent activities than the lead compound (1a) against H. pylori. Among them, compound 25a is 16-fold stronger (MIC = 0.39 mu g/mL) than 1a (MIC = 6.25 mu g/mL), and is even potent than the positive control metronidazole (MIC = 0.50 mu g/mL). The in vitro antimicrobial activities against H. pylori of these structurally diverse analogues based on the scaffold of la have also led to an outline of structure-activity relationship. (C) 2010 Elsevier Masson SAS. All rights reserved.
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