Spirocyclic Scaffolds in Drug Discovery

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Although spirocycles have been incorporated into drugs and explored in drug discovery for over five decades, recent years have seen a greater variety and number of spirocycles employed in drug discovery. This increase has been driven by improved synthetic methods, the quest for novel intellectual property, and the desirable, intrinsically three-dimensional nature of spirocycles. In this article, we discuss the conformational analysis of spirocycles, spirocyclic drugs, and selected examples of spirocyclic compounds from the medicinal chemistry literature.




Tice, C. M., Zheng, Y., & Singh, S. B. (2017). Spirocyclic Scaffolds in Drug Discovery. In Comprehensive Medicinal Chemistry III (Vol. 1–8, pp. 211–263). Elsevier Inc. https://doi.org/10.1016/B978-0-12-409547-2.12291-7

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