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Spirocyclic Scaffolds in Medicinal Chemistry.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Hiesinger K,Dar'in D,Proschak E,Krasavin M

doi

10.1021/acs.jmedchem.0c01473

subject

Has Abstract

pub_date

2021-01-14 00:00:00

pages

150-183

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

64

pub_type

杂志文章

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