作为和生物异构体的1,2-非替代双环[2.1.1] 素的基替代
Aleksandr Denisenko1, Pavel Garbuz1, Yelyzaveta Makovetska1
1Enamine Ltd Winston Churchill st. 78 02094 Kyiv Ukraine www.mykhailiukchem.org Pavel.Mykhailiuk@gmail.com.
新型双循环[2.1.1] 素作为和生物异构剂,用于整形替代的环. 这些化合物,当整合到杀菌剂中时,产生具有强大的抗真菌活性的无专利类型.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 农业化学品 农业化学品 农业化学品
背景情况:
- 整形替代环是生物活性分子中常见的图案.
- 开发新的生物异构体对于药物发现和规避专利至关重要.
- 现有的杀菌剂通常依赖于可能面临专利限制的芳香结构.
研究的目的:
- 合成和描述双环[2.1.1] 六作为和的生物异构体.
- 将bicyclo[2.1.1]hexane核心纳入已知的杀真菌剂结构中.
- 评估由此产生的类型的抗真菌活性和可专利性.
主要方法:
- 合成1,2-非替代的双环[2.1.1] 六衍生物.
- 使用光谱技术进行结构性表征.
- 对抗主要真菌病原体的抗真菌活性的生物评估.
- 对新型类似产品的专利环境的评估.
主要成果:
- 成功合成和表征双环[2.1.1] 六架.
- 证明双循环[2.1.1]hexanes作为有效的生物异构剂用于正位置换的环.
- 结合双循环[2.1.1] 六核的抗真菌类似物显示出高疗效.
- 发现这些新型类型的产品不受专利保护.
结论:
- 自行车[2.1.1]hexanes是可行的和生物异构体,用于正位替代的环.
- 开发的含有双循环[2.1.1]素的杀菌剂具有显著的抗真菌特性.
- 这种方法提供了一条通往新的,无需专利的农业化学解决方案的途径.
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