5- 烷基-1,2,3,4-四氢喹啉，由链霉菌和嗜热放线菌混合培养产生的新的具有膜相互作用的亲脂性代谢产物。
5-Alkyl-1,2,3,4-tetrahydroquinolines, new membrane-interacting lipophilic metabolites produced by combined culture of Streptomyces nigrescens and Tsukamurella pulmonis.
机构信息
†Department of System Chemotherapy and Molecular Sciences, Division of Bioinformatics and Chemical Genomics, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
‡Department of Biotechnology, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Bunkyo-ku, Tokyo 113-8657, Japan.
出版信息
Org Lett. 2015 Apr 17;17(8):1918-21. doi: 10.1021/acs.orglett.5b00607. Epub 2015 Mar 31.
Eight novel 5-alkyl-1,2,3,4-tetrahydroquinolines (5aTHQs) bearing different side chains have been isolated from a combined culture of Streptomyces nigrescens HEK616 and Tsukamurella pulmonis TP-B0596. The chemical structures including the absolute configuration were elucidated by spectroscopic analysis and total synthesis. 5aTHQs inhibited the growth of wild-type fission yeast while only weakly inhibiting the growth of several mutant strains synthesizing premature ergosterol. These results demonstrate that 5aTHQs are novel antifungals that may target cell membranes.
从一株链霉菌（Streptomyces nigrescens HEK616）和一株游动放线菌（Tsukamurella pulmonis TP-B0596）的混合发酵液中分离得到 8 个新型的 5-烷基-1,2,3,4-四氢喹啉（5aTHQs）衍生物，它们具有不同的侧链。通过光谱分析和全合成，确定了它们的化学结构和绝对构型。这些 5aTHQs 衍生物能够抑制野生型裂殖酵母的生长，而对合成前体麦角固醇的几种突变株的生长抑制作用较弱。这些结果表明，5aTHQs 可能是一种新型的抗真菌药物，作用靶点为细胞膜。
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