Spirocyclic Scaffolds in Medicinal Chemistry,Journal of Medicinal Chemistry

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Spirocyclic Scaffolds in Medicinal Chemistry
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-12-31 , DOI: 10.1021/acs.jmedchem.0c01473
Kerstin Hiesinger ₁ , Dmitry Dar’in ₂ , Ewgenij Proschak ₁ , Mikhail Krasavin ₂

Affiliation

Spirocyclic scaffolds are incorporated in various approved drugs and drug candidates. The increasing interest in less planar bioactive compounds has given rise to the development of synthetic methodologies for the preparation of spirocyclic scaffolds. In this Perspective, we summarize the diverse synthetic routes to obtain spirocyclic systems. The impact of spirocycles on potency and selectivity, including the aspect of stereochemistry, is discussed. Furthermore, we examine the changes in physicochemical properties as well as in in vitro and in vivo ADME using selected studies that compare spirocyclic compounds to their nonspirocyclic counterparts. In conclusion, the value of spirocyclic scaffolds in medicinal chemistry is discussed.

中文翻译：

药物化学中的螺环支架

螺环支架被并入各种批准的药物和候选药物中。对平面性较小的生物活性化合物的兴趣日益浓厚，引起了制备螺环支架的合成方法的发展。在此观点中，我们总结了获得螺环系统的各种合成途径。讨论了螺环对效能和选择性的影响，包括立体化学方面。此外，我们使用选定的比较螺环化合物与其非螺环化合物的研究，研究了理化性质以及体外和体内ADME的变化。总之，讨论了螺环支架在药物化学中的价值。

更新日期：2021-01-14

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