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三萜酸甲基哌嗪酰胺的合成、修饰及抗菌活性

[Synthesis, modifications, and antimicrobial activity of the methylpiperazinyl amides of triterpenic acids].

作者信息

Kazakova O B, Giniiatullina G V, Tolstikov G A, Medvedeva N I, Utkina T M, Kartashova O L

出版信息

Bioorg Khim. 2010 May-Jun;36(3):416-22. doi: 10.1134/s1068162010030155.

Abstract

N-Methylpiperazinyl amides of betulinic, platanic, glycyrrhetic, oleanolic, ursolic, and moronic acids were synthesized and modified. Betulin and betulonic acid showed antimicrobial activity against Staphylococcus aureus at a concentration of 90 mg/ml, and betulin manifested a bacteriostatic effect against Klebsiella pneumoniae at a concentration of 60 mg/ml. Among the studied N-methylpiperazinyl amides, the highest activity against S. aureus was observed for a betulonic acid derivative.

摘要

合成并修饰了桦木酸、悬铃木酸、甘草次酸、齐墩果酸、熊果酸和乌罗酸的N-甲基哌嗪基酰胺。桦木醇和桦木酮酸在浓度为90mg/ml时对金黄色葡萄球菌显示出抗菌活性,桦木醇在浓度为60mg/ml时对肺炎克雷伯菌表现出抑菌作用。在所研究的N-甲基哌嗪基酰胺中,观察到桦木酮酸衍生物对金黄色葡萄球菌的活性最高。

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