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Matthias R. Bauer, Paolo Di Fruscia, Simon C. C. Lucas, Iacovos N. Michaelides, Jennifer E. Nelson, R. Ian Storer, Benjamin C. Whitehurst
Aliphatic three- and four-membered rings including cyclopropanes, cyclobutanes, oxetanes, azetidines and bicyclo[1.1.1]pentanes have been increasingly exploited in medicinal chemistry for their beneficial physicochemical properties and applications as functional group bioisosteres. This review provides a historical perspective and comparative up to date overview of commonly applied small rings, exemplifying key principles with recent literature examples. In addition to describing the merits and advantages of each ring system, potential hazards and liabilities are also illustrated and explained, including any significant chemical or metabolic stability and toxicity risks.
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Bauer, M. R., Fruscia, P. D., Lucas, S. C. C., Michaelides, I. N., Nelson, J. E., Storer, R. I., & Whitehurst, B. C. (2021). Put a ring on it: application of small aliphatic rings in medicinal chemistry. RSC Medicinal Chemistry, 12(4), 448–471. https://doi.org/10.1039/d0md00370k
Bauer, Matthias R., et al. "Put a ring on it: application of small aliphatic rings in medicinal chemistry." RSC Medicinal Chemistry, vol. 12, no. 4, 2021, pp. 448–471, https://doi.org/10.1039/d0md00370k.
Bauer, Matthias R., Paolo Di Fruscia, Simon C. C. Lucas, Iacovos N. Michaelides, Jennifer E. Nelson, R. Ian Storer, and Benjamin C. Whitehurst. "Put a ring on it: application of small aliphatic rings in medicinal chemistry." RSC Medicinal Chemistry 12, no. 4 (2021): 448–471. https://doi.org/10.1039/d0md00370k.
Bauer M. R., Fruscia P. D., Lucas S. C. C. [и др.] Put a ring on it: application of small aliphatic rings in medicinal chemistry // RSC Medicinal Chemistry. — 2021. — Vol. 12, № 4. — P. 448–471. — URL: https://doi.org/10.1039/d0md00370k
@article{bauer2021ring,
title = {{Put a ring on it: application of small aliphatic rings in medicinal chemistry}},
author = {Matthias R. Bauer and Paolo Di Fruscia and Simon C. C. Lucas and Iacovos N. Michaelides and Jennifer E. Nelson and R. Ian Storer and Benjamin C. Whitehurst},
journal = {RSC Medicinal Chemistry},
year = {2021},
volume = {12},
number = {4},
pages = {448--471},
doi = {10.1039/d0md00370k},
url = {https://doi.org/10.1039/d0md00370k}
}TY - JOUR AU - Bauer, Matthias R. AU - Fruscia, Paolo Di AU - Lucas, Simon C. C. AU - Michaelides, Iacovos N. AU - Nelson, Jennifer E. AU - Storer, R. Ian AU - Whitehurst, Benjamin C. TI - Put a ring on it: application of small aliphatic rings in medicinal chemistry JO - RSC Medicinal Chemistry VL - 12 IS - 4 SP - 448 EP - 471 PY - 2021 DA - 2021/01/01 DO - 10.1039/d0md00370k UR - https://doi.org/10.1039/d0md00370k ER -
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