逃离平面国：[2 + 2]光环加成反应；用于先导化合物生成的构象受限富sp骨架
Escaping from Flatland: [2 + 2] Photocycloaddition; Conformationally Constrained sp-rich Scaffolds for Lead Generation.
作者信息
Cox Brian, Booker-Milburn Kevin I, Elliott Luke D, Robertson-Ralph Michael, Zdorichenko Victor
机构信息
School of Life Sciences, University of Sussex, Brighton, BN1 9QJ, U.K.
Photodiversity Ltd., c/o School of Life Sciences, University of Sussex, Brighton, BN1 9QJ, U.K.
出版信息
ACS Med Chem Lett. 2019 Oct 22;10(11):1512-1517. doi: 10.1021/acsmedchemlett.9b00409. eCollection 2019 Nov 14.
Abstract
Pressure on researchers to deliver new medicines to the patient continues to grow. Attrition rates in the research and development process present a significant challenge to the viability of the current model of drug discovery. Analysis shows that increasing the three-dimensionality of potential drug candidates decreases the risk of attrition, and it is for this reason many workers have taken a new look at the power of photochemistry, in particular photocycloadditions, as a means to generate novel sp-rich scaffolds for use in drug discovery programs. The viability of carrying out photochemical reactions on scale is also being addressed by the introduction of new technical developments.
摘要
向患者提供新药的研究人员所面临的压力持续增大。研发过程中的损耗率给当前药物发现模式的可行性带来了重大挑战。分析表明，增加潜在药物候选物的三维结构可降低损耗风险，正因如此，许多研究人员重新审视了光化学的力量，特别是光环加成反应，将其作为一种生成富含sp的新型骨架以用于药物发现项目的手段。新技术的发展也在解决大规模进行光化学反应的可行性问题。
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