Open Access
CC BY 4.0 · Pharmaceutical Fronts 2023; 05(01): e1-e14
DOI: 10.1055/s-0043-1764218
Review Article

Application of Chiral Piperidine Scaffolds in Drug Design

Qiu-Shi Chen
1   School of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai, People's Republic of China
2   Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, People's Republic of China
,
Jian-Qi Li
2   Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, People's Republic of China
,
Qing-Wei Zhang
2   Shanghai Institute of Pharmaceutical Industry Co., Ltd., China State Institute of Pharmaceutical Industry, Shanghai, People's Republic of China
› Author Affiliations

Funding We gratefully acknowledge financial supports from the National Science and Technology Major Project (Grant No. 2018ZX09711002-002-009), the National Natural Science Foundation of China (Grant No. 81703358), the Science and Technology Commission of Shanghai Municipality (Grant No. 17431903900, 18QB1404200, 21S11908000, 22ZR1460300), and the Graduate Innovation Fund Project of China State Institute of Pharmaceutical Industry (Grant No. YJS2021013, YJS2021011).


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Abstract

Chiral piperidine scaffolds are prevalent as the common cores of a large number of active pharmaceuticals in medical chemistry. This review outlined the diversity of chiral piperidine scaffolds in recently approved drugs, and also covers the scaffolds in leads and drug candidates. The significance of chiral piperidine scaffolds in drug design is also discussed in this article. With the introduction of chiral piperidine scaffolds into small molecules, the exploration of drug-like molecules can be benefitted from the following aspect: (1) modulating the physicochemical properties; (2) enhancing the biological activities and selectivity; (3) improving pharmacokinetic properties; and (4) reducing the cardiac hERG toxicity. Given above, chiral piperidine-based discovery of small molecules will be a promising strategy to enrich our molecules' library to fight against diseases.



Publication History

Received: 28 July 2022

Accepted: 26 January 2023

Article published online:
15 March 2023

© 2023. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting unrestricted use, distribution, and reproduction so long as the original work is properly cited. (https://creativecommons.org/licenses/by/4.0/)

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