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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Structural modification of a specific antimicrobial lead against Helicobacter pylori discovered from traditional Chinese medicine and a structure-activity relationship study.
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Structural modification of a specific antimicrobial lead against Helicobacter pylori discovered from traditional Chinese medicine and a structure-activity relationship study.

机译：中医发现幽门螺杆菌特异性抗菌铅的结构改性及结构 - 活性关系研究。

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摘要

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 1a 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 mug/mL) than 1a (MIC = 6.25 mug/mL), and is even potent than the positive control metronidazole (MIC = 0.50 mug/mL). The in vitro antimicrobial activities against H. pylori of these structurally diverse analogues based on the scaffold of 1a have also led to an outline of structure-activity relationship.
机译：发现Psoralen（1A）是来自在生物测定的中药（TCM）中的对幽门螺杆菌（H. Pylori）的特异性和有效的抗微生物引线。 因此，设计和合成了一系列结构不同的1A，以改善抗微生物效力，其中一些效力比铅化合物（1A）呈现更有效的活性。 其中，化合物25A更强（MIC = 0.39麦克风/ m1），比1a（MIC = 6.25麦克风/ mL）更强，并且甚至比阳性对照核苷唑（MIC = 0.50麦克风/ mL）有效。 基于1A支架的这些结构多样性类似物的对幽门螺杆菌的体外抗微生物活性也导致了结构 - 活性关系的轮廓。

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