Key Laboratory of Marine Drugs, The Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
Department of Chemistry, Women University Swabi, Swabi 23430, Pakistan.
Mar Drugs. 2022 Jan 18;20(2):82. doi: 10.3390/md20020082.
To enhance the biological activity of the natural product geodin (), isolated from the marine-derived fungus sp., a series of new ether derivatives (-) was designed and semisynthesized using a high-yielding one-step reaction. In addition, the insecticidal and antibacterial activities of all geodin congeners were evaluated systematically. Most of these derivatives showed better insecticidal activities against Hübner than . In particular, showed potent insecticidal activity with an IC value of 89 μM, comparable to the positive control azadirachtin (IC = 70 μM). Additionally, , , , , and showed strong antibacterial activity against and with MIC values in the range of 1.15-4.93 μM. The preliminary structure-activity relationships indicated that the introduction of halogenated benzyl especially fluorobenzyl, into and substitution of 4-OH could be key factors in increasing the insecticidal and antibacterial activities of geodin.
为了提高天然产物 geodin（）的生物活性，该化合物从海洋来源的真菌 sp. 中分离得到，我们设计并使用高产一步反应半合成了一系列新的醚衍生物（-）。此外，我们还系统地评估了所有 geodin 同系物的杀虫和抗菌活性。这些衍生物大多数对 Hübner 的杀虫活性优于 。特别是 表现出很强的杀虫活性，IC 值为 89 μM，与阳性对照印苦素（IC = 70 μM）相当。此外， 、 、 、 、 对 和 具有很强的抗菌活性，MIC 值在 1.15-4.93 μM 范围内。初步的结构-活性关系表明，在 和 中引入卤化苄基（特别是氟苄基）以及取代 4-OH 可能是提高 geodin 杀虫和抗菌活性的关键因素。
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