دورية أكاديمية
Design, Semisynthesis, Insecticidal and Antibacterial Activities of a Series of Marine-Derived Geodin Derivatives and Their Preliminary Structure–Activity Relationships
| العنوان: | Design, Semisynthesis, Insecticidal and Antibacterial Activities of a Series of Marine-Derived Geodin Derivatives and Their Preliminary Structure–Activity Relationships |
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| المؤلفون: | Rong Chao, Gulab Said, Qun Zhang, Yue-Xuan Qi, Jie Hu, Cai-Juan Zheng, Ji-Yong Zheng, Chang-Lun Shao, Guang-Ying Chen, Mei-Yan Wei |
| المصدر: | Marine Drugs, Vol 20, Iss 2, p 82 (2022) |
| بيانات النشر: | MDPI AG, 2022. |
| سنة النشر: | 2022 |
| المجموعة: | LCC:Biology (General) |
| مصطلحات موضوعية: | Aspergillus sp., geodin, semisynthesize, insecticidal activity, antibacterial activity, Biology (General), QH301-705.5 |
| الوصف: | To enhance the biological activity of the natural product geodin (1), isolated from the marine-derived fungus Aspergillus sp., a series of new ether derivatives (2–37) 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 Helicoverpa armigera Hübner than 1. In particular, 15 showed potent insecticidal activity with an IC50 value of 89 μM, comparable to the positive control azadirachtin (IC50 = 70 μM). Additionally, 5, 12, 13, 16, 30 and 33 showed strong antibacterial activity against Staphylococcus aureus and Aeromonas salmonicida 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 1 and substitution of 4-OH could be key factors in increasing the insecticidal and antibacterial activities of geodin. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 20020082 1660-3397 |
| Relation: | https://www.mdpi.com/1660-3397/20/2/82; https://doaj.org/toc/1660-3397 |
| DOI: | 10.3390/md20020082 |
| URL الوصول: | https://doaj.org/article/330300479f964de4abc7183b86b2d6d6 |
| رقم الأكسشن: | edsdoj.330300479f964de4abc7183b86b2d6d6 |
| قاعدة البيانات: | Directory of Open Access Journals |
Full Text Finder | تدمد: | 20020082 16603397 |
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| DOI: | 10.3390/md20020082 |