The DOI matches its Crossref record; 101 of the 101 references it cites were found in a registry or an index.
The Necessary Nitrogen Atom: A Versatile High-Impact Design Element for Multiparameter Optimization
Open accessAbstract
There is a continued desire in biomedical research to reduce the number and duration of design cycles required to optimize lead compounds into high-quality chemical probes or safe and efficacious drug candidates. The insightful application of impactful molecular design elements is one approach toward achieving this goal. The replacement of a CH group with a N atom in aromatic and heteroaromatic ring systems can have many important effects on molecular and physicochemical properties and intra- and intermolecular interactions that can translate to improved pharmacological profiles. In this Perspective, the "necessary nitrogen atom" is shown to be a versatile high-impact design element for multiparameter optimization, wherein ≥10-, 100-, or 1000-fold improvement in a variety of key pharmacological parameters can be realized.
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Cites
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Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design
Subbaiah, M. A. M., & Meanwell, N. A. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01215 · Cited by 710
Shultz, M. D. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00686 · Cited by 434
Pratley, C., Fenner, S., & Murphy, J. A. (2022) · Chemical Reviews · doi:10.1021/acs.chemrev.1c00831 · Cited by 422
The Expanding Role of Pyridine and Dihydropyridine Scaffolds in Drug Design
Ling, Y., Hao, Z.-Y., Liang, D., Zhang, C.-L., Liu, Y.-F., & Wang, Y. (2021) · Drug Design, Development and Therapy · doi:10.2147/dddt.s329547 · Cited by 414
Clark, A. J., Negron, C., Hauser, K., Sun, M., Wang, L., Abel, R., & Friesner, R. A. (2019) · Journal of Molecular Biology · doi:10.1016/j.jmb.2019.02.003 · Cited by 91
Metadata
- Authors
- Pennington, L. D., & Moustakas, D. T.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2017-02-08
- Volume
- 60
- Issue
- 9
- Pages
- 3552-3579
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2587696209
- Cited by
- 408
- References
- 101
- FWCI
- 16.95
- Type
- journal article
- Language
- en
- Open access
- green
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- Pennington, L. D., & Moustakas, D. T. (2017). The Necessary Nitrogen Atom: A Versatile High-Impact Design Element for Multiparameter Optimization. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.6b01807
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
