The DOI matches its Crossref record; 79 of the 79 references it cites were found in a registry or an index.
Applications of Deuterium in Medicinal Chemistry
Abstract
The use of deuteration in medicinal chemistry has exploded in the past years, and the FDA has recently approved the first deuterium-labeled drug. Precision deuteration goes beyond the pure and simple amelioration of the pharmacokinetic parameters of a drug and might provide an opportunity when facing problems in terms of metabolism-mediated toxicity, drug interactions, and low bioactivation. The use of deuterium is even broader, offering the opportunity to lower the degree of epimerization, reduce the dose of coadministered boosters, and discover compounds where deuterium is the basis for the mechanism of action. Nevertheless, designing, synthesizing, and developing a successful deuterated drug is far from straightforward, and the translation from concept to practice is often unpredictable. This Perspective provides an overview of the recent developments of deuteration, with a focus on deuterated clinical candidates, and highlights both opportunities and challenges of this strategy.
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Cites
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Cited by
U.S. FDA Approved Drugs from 2015–June 2020: A Perspective
Bhutani, P., Joshi, G., Raja, N., Bachhav, N., Rajanna, P. K., Bhutani, H., Paul, A. T., & Kumar, R. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01786 · Cited by 815
Turcu, A. L., Companys-Alemany, J., Phillips, M. B., Patel, D. S., Griñán-Ferré, C., Loza, M. I., Brea, J. M., Pérez, B., Soto, D., Sureda, F. X., et al. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114354 · Cited by 27
Chen, M. C., Korth, C. C., Harnett, M. D., Elenko, E., & Lickliter, J. D. (2022) · Clinical Pharmacology in Drug Development · doi:10.1002/cpdd.1040 · Cited by 18
Metadata
- Authors
- Pirali, T., Serafini, M., Cargnin, S., & Genazzani, A. A.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2019-01-14
- Volume
- 62
- Issue
- 11
- Pages
- 5276-5297
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2909275830
- Cited by
- 855
- References
- 79
- FWCI
- 27.52
- Type
- journal article
- Language
- en
- Open access
- closed
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- Pirali, T., Serafini, M., Cargnin, S., & Genazzani, A. A. (2019). Applications of Deuterium in Medicinal Chemistry. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.8b01808
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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