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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：从中药中发现的针对幽门螺杆菌的特定抗菌剂的结构修饰以及结构-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：补骨脂素（1a）是针对生物测定法的直接分离中来自传统中药（TCM）的幽门螺杆菌（H. pylori）的一种特异性和有效的抗菌药。因此，设计并合成了一系列结构不同的1a类似物，以提高抗菌效力，其中一些表现出比针对幽门螺杆菌的先导化合物（1a）更强的活性。其中，化合物25a（MIC = 0.39杯/毫升）比1a（MIC = 6.25杯/毫升）强16倍，甚至比阳性对照甲硝唑（MIC = 0.50杯/毫升）强。这些基于1a支架的结构多样的类似物对幽门螺杆菌的体外抗菌活性也导致了构效关系的概述。

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