Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores
Sean W Reilly
1
,
Suzy Griffin
2
,
M. M. Taylor
2
,
Kristoffer Sahlholm
1
,
Chi-Chang Weng
1
,
Kuiying Xu
1
,
Daniel A. Jacome
3
,
Robert R. Luedtke
2
,
Robert H. Mach
1
Publication type: Journal Article
Publication date: 2017-11-21
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
29125762
Drug Discovery
Molecular Medicine
Abstract
A series of potent and selective D3 receptor (D3R) analogues with diazaspiro alkane cores were synthesized. Radioligand binding of compounds 11, 14, 15a, and 15c revealed favorable D3R affinity (Ki = 12-25.6 nM) and were highly selective for D3R vs D3R (ranging from 264- to 905-fold). Variation of these novel ligand architectures can be achieved using our previously reported 10-20 min benchtop C-N cross-coupling methodology, affording a broad range of arylated diazaspiro precursors.
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Metrics
33
Total citations:
33
Citations from 2025:
2
(6.06%)
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MLA
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GOST
Copy
Reilly S. W. et al. Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores // Journal of Medicinal Chemistry. 2017. Vol. 60. No. 23. pp. 9905-9910.
GOST all authors (up to 50)
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Reilly S. W., Griffin S., Taylor M. M., Sahlholm K., Weng C., Xu K., Jacome D. A., Luedtke R. R., Mach R. H. Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores // Journal of Medicinal Chemistry. 2017. Vol. 60. No. 23. pp. 9905-9910.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1021/acs.jmedchem.7b01248
UR - https://doi.org/10.1021/acs.jmedchem.7b01248
TI - Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores
T2 - Journal of Medicinal Chemistry
AU - Reilly, Sean W
AU - Griffin, Suzy
AU - Taylor, M. M.
AU - Sahlholm, Kristoffer
AU - Weng, Chi-Chang
AU - Xu, Kuiying
AU - Jacome, Daniel A.
AU - Luedtke, Robert R.
AU - Mach, Robert H.
PY - 2017
DA - 2017/11/21
PB - American Chemical Society (ACS)
SP - 9905-9910
IS - 23
VL - 60
PMID - 29125762
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2017_Reilly,
author = {Sean W Reilly and Suzy Griffin and M. M. Taylor and Kristoffer Sahlholm and Chi-Chang Weng and Kuiying Xu and Daniel A. Jacome and Robert R. Luedtke and Robert H. Mach},
title = {Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores},
journal = {Journal of Medicinal Chemistry},
year = {2017},
volume = {60},
publisher = {American Chemical Society (ACS)},
month = {nov},
url = {https://doi.org/10.1021/acs.jmedchem.7b01248},
number = {23},
pages = {9905--9910},
doi = {10.1021/acs.jmedchem.7b01248}
}
Cite this
MLA
Copy
Reilly, Sean W., et al. “Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores.” Journal of Medicinal Chemistry, vol. 60, no. 23, Nov. 2017, pp. 9905-9910. https://doi.org/10.1021/acs.jmedchem.7b01248.