设计,合成和生物评估具有不同程度的分子复杂度的平坦西米辛类似物
K C Nicolaou1, Antonia F Stepan, Troy Lister
1Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA. kcn@scripps.edu
Journal of the American Chemical Society
|September 6, 2008
概括
研究人员探索了白胺类类似物,发现酸部分对活性至关重要,但四环可以改变而不会失去抗生素功能.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 药理学 药理学 是一个学科.
背景情况:
- 普拉西米辛是一种具有复杂结构的新型抗生素.
- 了解其结构-活性关系是开发新抗生素的关键.
研究的目的:
- 为了合成和生物评估平坦西米辛类似物.
- 确定酸和四环域对生物活性的重要性.
主要方法:
- 分子设计和化学合成两个系列的platensimycin类似物.
- 合成化合物的生物评估,以评估抗菌活性.
主要成果:
- 替代的酸部分对化的活性至关重要,需要特定的功能组.
- 四环域可以经历显著的结构修改,而不会影响生物作用.
结论:
- 酸域是一个高度保存的药元素.
- 四环提供灵活性,用于设计下一代平坦西米辛类似物.
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