环状八肽伯克霍尔德菌素类似物的合成及抗真菌活性。
Synthesis and antifungal activities of cyclic octa-lipopeptide burkholdine analogues.
机构信息
Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, 4-3-16 Jonan, Yonezawa, Yamagata 992-8510, Japan.
出版信息
Bioorg Med Chem Lett. 2013 Jul 15;23(14):4244-7. doi: 10.1016/j.bmcl.2013.04.091. Epub 2013 May 14.
Synthesis and antifungal activity of cyclic octapeptide derivatives of burkholdines are described. To construct cyclic octapeptides, the combination of Fmoc-SPPS and cyclization with DIC/HOBt in the solution phase was employed. Synthesized peptides were evaluated for antifungal activity with MIC values against Saccharomyces cerevisiae, Aspergillus oryzae, and Candida viswanathii. As a result, the lipid side chain and the stereochemistry of each amino acid of Bk-1097 analogues significantly affected antifungal activity.
本文描述了伯克霍尔德菌素的环状八肽衍生物的合成和抗真菌活性。为了构建环状八肽，采用 Fmoc-SPPS 与 DIC/HOBt 在溶液相中的环化相结合的方法。合成的肽进行了抗真菌活性评估，MIC 值针对酿酒酵母、米曲霉和粘红酵母。结果表明，Bk-1097 类似物的脂质侧链和每个氨基酸的立体化学显著影响抗真菌活性。
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