Synthesis and Biological Evaluation of a Beauveriolide Analogue Library
| العنوان: | Synthesis and Biological Evaluation of a Beauveriolide Analogue Library |
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| المؤلفون: | Takayuki Doi, Satoshi Ōmura,‡,§ and, Hiroshi Tomoda, Toshiaki Sunazuka, Kenichiro Nagai, Takashi Takahashi, Takafumi Sekiguchi, Ichiji Namatame |
| المصدر: | Journal of Combinatorial Chemistry. 8:103-109 |
| بيانات النشر: | American Chemical Society (ACS), 2005. |
| سنة النشر: | 2005 |
| مصطلحات موضوعية: | Depsipeptide, Molecular Structure, Stereochemistry, General Chemistry, Beauveriolide III, High-performance liquid chromatography, Combinatorial chemistry, Lipid droplet accumulation, Mice, Structure-Activity Relationship, chemistry.chemical_compound, chemistry, Cyclization, Depsipeptides, Macrophages, Peritoneal, Animals, Combinatorial Chemistry Techniques, Cholesterol Esters, Linker, Chromatography, High Pressure Liquid, Derivative (chemistry), Hypolipidemic Agents, Biological evaluation |
| الوصف: | Synthesis of beauveriolide III (1b), which is an inhibitor of lipid droplet accumulation in macrophages, was achieved by solid-phase assembly of linear depsipeptide using a 2-chlorotrityl linker followed by solution-phase cyclization. On the basis of this strategy, a combinatorial library of beauveriolide analogues was carried out by radio frequency-encoded combinatorial chemistry. After automated purification using preparative reversed-phase HPLC, the library was tested for inhibitory activity of CE synthesis in macrophages to determine structure-activity relationships of beauveriolides. Among them, we found that diphenyl derivative 7{9,1} is 10 times more potent than 1b. |
| تدمد: | 1520-4774 1520-4766 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d768ad4950351c0da442cfc0727ce1eaTest https://doi.org/10.1021/cc050084dTest |
| رقم الانضمام: | edsair.doi.dedup.....d768ad4950351c0da442cfc0727ce1ea |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15204774 15204766 |
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