3-多氨基-23,24-双降胆烷作为甾体-多胺缀合物的简明合成及抗菌活性。
A concise synthesis and antimicrobial activities of 3-polyamino-23,24-bisnorcholanes as steroid-polyamine conjugates.
机构信息
Department of Applied Chemistry, Kyungpook National University, Daegu 702-701, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2011 Jul 1;21(13):3861-5. doi: 10.1016/j.bmcl.2011.05.048. Epub 2011 May 24.
A series of steroid-polyamine conjugates were synthesized and evaluated for their antimicrobial activity. This study was focused on the effect of stereochemistry at the C-3 and C-5 of steroids and types of polyamine at C-3 on activity against various human pathogens. All the conjugates exhibited strong antimicrobial activities against Gram-positive strains. Compound 18 was found to be the most potent in these series with a MIC value as low as 1 μg/mL against the bacterium Staphylococcus aureus ATCC6538P.
合成了一系列甾体-多胺缀合物，并评估了它们的抗菌活性。本研究重点研究了甾体 C-3 和 C-5 立体化学以及 C-3 位多胺类型对各种人类病原体活性的影响。所有缀合物均表现出对革兰氏阳性菌株的强抗菌活性。在这些系列中，化合物 18 的活性最强，对金黄色葡萄球菌 ATCC6538P 的 MIC 值低至 1μg/mL。
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