相关实验视频
Updated: Jul 16, 2026

11:10
Expression, Purification, and Antimicrobial Activity of S100A12
Published on: May 13, 2017
合成抗真菌的宏类抗生素 (+) - 罗克萨素
David A Evans1, Brian T Connell
1Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA. Evans@Chemistry.Harvard.edu
Journal of the American Chemical Society
|September 4, 2003
概括
抗真菌宏类抗生素罗沙的总合成是使用阿尔多尔和还原步骤实现的. 关键片段被合,然后进行功能化和乳化,以完成罗沙的结构.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 自然产品的合成自然产品的合成
背景情况:
- 罗克萨是一种具有抗真菌性能的宏类抗生素.
- 罗克萨的复杂结构构成了重要的合成挑战.
研究的目的:
- 为了实现抗真菌类抗生素罗克萨的总合成.
- 开发一个高效和融合的合成路线.
主要方法:
- 利用阿尔多尔和定向还原反应来构建聚醇骨干.
- 用于碎片合的朱莉亚化和甲基醇添加物.
- 通过功能化反应结合了敏感的聚烯部分.
主要成果:
- 通过融合方法成功合成了罗克萨西.
- 在乳化阶段取得了良好的产量.
- 通过酸性降低保护完成了合成.
结论:
- 罗克萨提辛的总合成已经成功完成.
- 开发的合成策略对于构建复杂的类抗生素是有效的.
相关概念视频
Combined Effects of Drugs: Synergism
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
Production of Antibiotics
Penicillin, one of the earliest and most widely used antibiotics, is produced industrially by the filamentous fungus Penicillium chrysogenum. Large stirred-tank bioreactors ranging from tens to hundreds of thousands of liters maintain tightly controlled temperature, pH, and dissolved oxygen conditions to support fungal metabolism and maximize antibiotic yield. Penicillin is a secondary metabolite, synthesized primarily during the stationary growth phase, which requires a carefully managed...
Microbiota Modulation by Antibiotics
Antibiotics have revolutionized modern medicine by saving countless lives from bacterial infections. However, their widespread use has inadvertently harmed the delicate balance of the human gut microbiota. The gut microbiota, a complex community of bacteria, archaea, viruses, and fungi, plays a vital role in regulating metabolism, immune responses, and maintaining intestinal health. Antibiotics, especially broad-spectrum types, disrupt this ecosystem by eradicating both harmful and beneficial...
Inhibitors of Gram-positive Cell Wall Synthesis
Bacterial cell walls are typically rigid structures composed mainly of peptidoglycan, a mesh-like polymer that provides mechanical strength and maintains cell shape. The synthesis of peptidoglycan is a crucial process in bacterial growth and serves as a primary target for many antibiotics.Mechanism of Action of Beta-Lactam AntibioticsBeta-lactam antibiotics, such as penicillin, inhibit peptidoglycan synthesis in actively growing cells. These antibiotics share a characteristic four-membered...
Inhibitors of Bacterial Protein Synthesis
Aminoglycosides constitute a highly potent class of bactericidal antibiotics that exert their antimicrobial effects by targeting the bacterial ribosome, specifically disrupting protein synthesis. These polycationic molecules consist of amino-modified sugars linked via glycosidic bonds to an aminocyclitol core such as 2-deoxystreptamine or streptamine. Their strong positive charges facilitate tight binding to the negatively charged phosphate backbone of ribosomal RNA (rRNA), primarily at the 16S...
Clinical Significance of Antibiotic Resistance
Methicillin-resistant Staphylococcus aureus (MRSA) presents a critical public health threat, arising from its capacity to resist β-lactam antibiotics due to acquisition of the mecA gene within the staphylococcal cassette chromosome mec (SCCmec). This gene encodes penicillin-binding protein 2a (PBP2a), which impairs binding efficacy of methicillin and other β-lactams. MRSA has evolved into distinct clonal lineages impacting humans and animals alike, reinforcing its significance within the One...

