{"title":"Synthesis of drimanyl indole fragments of drimentine alkaloids and their antibacterial activities.","authors":"Jili Feng, Nini Qu, Summia Kalsoom, Zunjun Zhou, Shiyi Zhang, Zhe Cui, Chongmin Zhong, Miaofeng Ma","doi":"10.1016/j.bmcl.2024.130040","DOIUrl":null,"url":null,"abstract":"<p><p>Two types of drimanyl indole fragments of drimentine alkaloids were synthesized and evaluated their in vitro antibacterial activities using minimum inhibitory concentration. Analysis of structure-activity relationship against Ralstonia solanacearum revealed that fragment I exhibited superior inhibitory activity compared to fragment II. Notably, free NH of the indole motif was essential for antibacterial activity, while C<sup>12</sup>OH of the drimane skeleton was beneficial for enhancing the inhibitory effect. Compound 2, possessing these structural features, showed the highest activity to R. solanacearum among all the tested compounds with a MIC value of 8 µg/mL, indicating its potential as a promising lead for the development of novel antibiotics.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130040"},"PeriodicalIF":2.5000,"publicationDate":"2024-11-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.bmcl.2024.130040","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Two types of drimanyl indole fragments of drimentine alkaloids were synthesized and evaluated their in vitro antibacterial activities using minimum inhibitory concentration. Analysis of structure-activity relationship against Ralstonia solanacearum revealed that fragment I exhibited superior inhibitory activity compared to fragment II. Notably, free NH of the indole motif was essential for antibacterial activity, while C12OH of the drimane skeleton was beneficial for enhancing the inhibitory effect. Compound 2, possessing these structural features, showed the highest activity to R. solanacearum among all the tested compounds with a MIC value of 8 µg/mL, indicating its potential as a promising lead for the development of novel antibiotics.
drimanyl indole fragments of drimentine alkaloids and their antibacterial activities.
研究人员合成了两种地米星生物碱的地米酰吲哚片段，并利用最小抑菌浓度评估了它们的体外抗菌活性。对茄属拉氏菌（Ralstonia solanacearum）的结构-活性关系分析表明，与片段 II 相比，片段 I 表现出更强的抑制活性。值得注意的是，吲哚基团的游离 NH 是抗菌活性的关键，而二氢大麻烷骨架的 C12OH 则有利于增强抑菌效果。具有这些结构特征的化合物 2 在所有测试化合物中对 R. solanacearum 的活性最高，其 MIC 值为 8 µg/mL，这表明它有望成为开发新型抗生素的先导化合物。
期刊介绍：
Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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