The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals: Miniperspective
Abstract
Nitrogen heterocycles are among the most significant structural components of pharmaceuticals. Analysis of our database of U.S. FDA approved drugs reveals that 59% of unique small-molecule drugs contain a nitrogen heterocycle. In this review we report on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals. The main part of our analysis is divided into seven sections: (1) three- and four-membered heterocycles, (2) five-, (3) six-, and (4) seven- and eight-membered heterocycles, as well as (5) fused, (6) bridged bicyclic, and (7) macrocyclic nitrogen heterocycles. Each section reveals the top nitrogen heterocyclic structures and their relative impact for that ring type. For the most commonly used nitrogen heterocycles, we report detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.
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Cites
Oral Sildenafil in the Treatment of Erectile Dysfunction
Goldstein, I., Lue, T. F., Padma-Nathan, H., Rosen, R. C., Steers, W. D., & Wicker, P. A. (1998) · New England Journal of Medicine · doi:10.1056/nejm199805143382001 · Cited by 2,120
Cited by
Contribution of Organofluorine Compounds to Pharmaceuticals
Inoue, M., Sumii, Y., & Shibata, N. (2020) · ACS Omega · doi:10.1021/acsomega.0c00830 · Cited by 1,944
Bayesian reaction optimization as a tool for chemical synthesis
Shields, B. J., Stevens, J., Li, J., Parasram, M., Damani, F., Alvarado, J. I. M., Janey, J. M., Adams, R. P., & Doyle, A. G. (2021) · Nature · doi:10.1038/s41586-021-03213-y · Cited by 1,063
Predicting reaction performance in C–N cross-coupling using machine learning
Ahneman, D. T., Estrada, J. G., Lin, S., Dreher, S. D., & Doyle, A. G. (2018) · Science · doi:10.1126/science.aar5169 · Cited by 1,058
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
The importance of synthetic chemistry in the pharmaceutical industry
Campos, K. R., Coleman, P. J., Alvarez, J. C., Dreher, S. D., Garbaccio, R. M., Terrett, N. K., Tillyer, R. D., Truppo, M. D., & Parmee, E. R. (2019) · Science · doi:10.1126/science.aat0805 · Cited by 668
Metadata
- Authors
- Vitaku, E., Smith, D. T., & Njardarson, J. T.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2014-10-07
- Volume
- 57
- Issue
- 24
- Pages
- 10257-10274
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2407040666
- Cited by
- 6,418
- References
- 1
- FWCI
- 154.40
- Type
- journal article
- Language
- en
- Open access
- closed
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