具有医学意义的-异芳香基的酶选择性生物还原
Wen-Ju Bai1, Michelle A Estrada1, Jackson A Gartman1
1AbbVie Inc., North Chicago, Illinois 60064, United States.
ACS medicinal chemistry letters
|June 14, 2023
概括
这项研究提出了使用紫色胡卜的-异芳香基的新型enantioselective生物减少方法. 这种方法提供了一个可扩展和高效的工具,用于合成在药物发现中至关重要的奇拉醇.
科学领域:
- 有机化学 有机化学
- 生物催化剂是一种生物催化剂.
- 药用化学 医学化学
背景情况:
- 亚洲食品和药物管理局批准的药物中异芳香物很普遍.
- 有效合成含有这些异环的性酒精对于药物开发至关重要.
- 现有的合成这些化合物的方法可能在范围或可扩展性方面受到限制.
研究的目的:
- 开发一种对携带常见-异芳素的子进行enantioselective生物还原方法.
- 扩大植物媒介减肥的基质范围.
- 为药物化学家提供一个实用且可扩展的工具.
主要方法:
- 在缓冲水性介质中使用紫色胡卜作为生物催化剂.
- 在生物还原过程中采用了简化的反应组合.
- 研究了十种含的异环环.
主要成果:
- 在周围环境温度下,在48小时内实现异芳基的酶选择生物还原.
- 成功扩大了基质范围,耐受了七种新型的异环环.
- 证明了该方法的有效性,使用广泛的结构多样化的性酒精.
结论:
- 植物介导的生物还原为合成有价值的性酒精提供了一种务实的,可扩展的方法.
- 这种方法通过提供访问各种构建块来加速药物化学活动.
- 开发的生物催化转化扩大了在药物合成中植物媒介减量的实用性.
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