Spirocyclic Scaffolds in Medicinal Chemistry
Publication type: Journal Article
Publication date: 2020-12-31
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
33381970
Drug Discovery
Molecular Medicine
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.
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Metrics
482
Total citations:
482
Citations from 2024:
275
(57.29%)
Cite this
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MLA
Cite this
GOST
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Hiesinger K. et al. Spirocyclic Scaffolds in Medicinal Chemistry // Journal of Medicinal Chemistry. 2020. Vol. 64. No. 1. pp. 150-183.
GOST all authors (up to 50)
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Hiesinger K., Dar’in D., Proschak E., Novikov A. S. Spirocyclic Scaffolds in Medicinal Chemistry // Journal of Medicinal Chemistry. 2020. Vol. 64. No. 1. pp. 150-183.
Cite this
RIS
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TY - JOUR
DO - 10.1021/acs.jmedchem.0c01473
UR - https://doi.org/10.1021/acs.jmedchem.0c01473
TI - Spirocyclic Scaffolds in Medicinal Chemistry
T2 - Journal of Medicinal Chemistry
AU - Hiesinger, Kerstin
AU - Dar’in, Dmitry
AU - Proschak, Ewgenij
AU - Novikov, Alexander S.
PY - 2020
DA - 2020/12/31
PB - American Chemical Society (ACS)
SP - 150-183
IS - 1
VL - 64
PMID - 33381970
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2020_Hiesinger,
author = {Kerstin Hiesinger and Dmitry Dar’in and Ewgenij Proschak and Alexander S. Novikov},
title = {Spirocyclic Scaffolds in Medicinal Chemistry},
journal = {Journal of Medicinal Chemistry},
year = {2020},
volume = {64},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/acs.jmedchem.0c01473},
number = {1},
pages = {150--183},
doi = {10.1021/acs.jmedchem.0c01473}
}
Cite this
MLA
Copy
Hiesinger, Kerstin, et al. “Spirocyclic Scaffolds in Medicinal Chemistry.” Journal of Medicinal Chemistry, vol. 64, no. 1, Dec. 2020, pp. 150-183. https://doi.org/10.1021/acs.jmedchem.0c01473.